KRN 7000: has an alpha-galactosylceramide structure; structure given in first source [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]
alpha-galactosylceramide : A galactosylceramide in which the galactosyl residue has alpha anomeric conofiguration. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
1-O-(alpha-D-galactosyl)-N-hexacosanoylphytosphingosine : A glycophytoceramide having an alpha-D-galactosyl residue at the O-1 position and a hexacosanoyl group attached to the nitrogen. [Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res]
| ID Source | ID |
|---|---|
| PubMed CID | 2826713 |
| CHEMBL ID | 384200 |
| CHEBI ID | 466659 |
| SCHEMBL ID | 512949 |
| MeSH ID | M0271479 |
| Synonym |
|---|
| wx671898jf , |
| unii-wx671898jf |
| rgi-2001 |
| n-[(2s,3s,4r)-3,4-dihydroxy-1-[(2s,3r,4s,5r,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxyoctadecan-2-yl]hexacosanamide |
| agl-582 |
| alpha-galactosylceramide |
| krn-7000 |
| alpha-galcer |
| krn 7000 |
| hexacosanamide, n-[(1s,2s,3r)-1-[(alpha-d-galactopyranosyloxy)methyl]-2,3-dihydroxyheptadecyl]- (9ci) |
| hexacosanamide, n-[1-[(alpha-d-galactopyranosyloxy)methyl]-2,3-dihydroxyheptadecyl]-, [1s-(1r*,2r*,3s*)]- |
| 158021-47-7 |
| chemid158021477 |
| ccris 8968 |
| hexacosanamide, n-[(1s,2s,3r)-1-[(alpha-d-galactopyranosyloxy)methyl]-2,3-dihydroxyheptadecyl]- |
| n-{(1s,2r,3s)-1-[(alpha-d-galactopyranosyloxy)methyl]-2,3-dihydroxyheptadecyl}hexacosanamide |
| n-((2s,3s,4r)-3,4-dihydroxy-1-(3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2h-pyran-2-yloxy)octadecan-2-yl)hexaicosanamide |
| krn7000 |
| hexacosanamide, n-(1-((alpha-d-galactopyranosyloxy)methyl)-2,3-dihdyroxyheptadecyl)-, (1s-(1r*,2r*,3s*))- |
| alpha-galactosyl ceramide |
| alpha-gc(c26) |
| 1-o-(alpha-d-galactopyranosyl)-n-hexacosanoylphytosphingosine |
| CHEBI:466659 , |
| alpha-gc (c26) |
| alpha-galcer(t18:0/26:0) |
| 1-o-(alpha-d-galactosyl)-n-hexacosanoylphytosphingosine |
| galalpha-cer(t18:0/26:0) |
| (2s,3s,4r)-1-o-(alpha-d-galactosyl)-n-hexacosanoyl-2-amino-1,3,4-octadecanetriol |
| n-[(2s,3s,4r)-1-(alpha-d-galactopyranosyloxy)-3,4-dihydroxyoctadecan-2-yl]hexacosanamide |
| rgi-7000 |
| .alpha.-galcer |
| CHEMBL384200 |
| C16892 |
| |a-galactosylceramide |
| EPITOPE ID:130694 |
| hexacosanamide, n-((1s,2s,3r)-1-((.alpha.-d-galactopyranosyloxy)methyl)-2,3-dihydroxyheptadecyl)- |
| SCHEMBL512949 |
| AC-31508 |
| (2s,3s,4r)-1-o-(alpha-d-galactosyl)-n-hexacosanoyl-2-amino-1,3,4-octadecanetriol, >=95% (tlc) |
| VQFKFAKEUMHBLV-BYSUZVQFSA-N |
| DB12232 |
| n-{(1s,2s,3r)-1-[(alpha-d-galactopyranosyloxy)methyl]-2,3-dihydroxyheptadecyl}hexacosanamide |
| mfcd00939559 |
| DTXSID40935847 |
| Q27105159 |
| EX-A5755 |
| n-((2s,3s,4r)-3,4-dihydroxy-1-(((2s,3r,4s,5r,6r)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2h-pyran-2-yl)oxy)octadecan-2-yl)hexacosanamide |
| alpha-galactosylceramide(a-gal-cer) (synthetic) |
| -galcer;krn7000 |
| -galactosylceramide |
| GLXC-26234 |
| AKOS040741093 |
| ??-galactosylceramide |
| Excerpt | Reference | Relevance |
|---|---|---|
| " It was validated that adding bile salts to the system boosted intestinal lymphatic transport as well as the oral bioavailability of ovalbumin (OVA) via the chylomicron pathway." | ( Oral lymphatic delivery of alpha-galactosylceramide and ovalbumin evokes anti-cancer immunization. Cho, SS; Cho, YC; Choi, JU; Kim, KT; Kim, SH; Kim, Y; Mujahid, K; Pandey, P; Park, JW; Shim, JH; Subedi, L, 2023) | 0.91 |
| Excerpt | Relevance | Reference |
|---|---|---|
| " These data indicate that prudent discussion is required to determine the dosing interval of alpha-GalCer in clinical applications." | ( [Repeated administration of alpha-galactosyl ceramide attenuates of natural killer T cells]. Hatakeyama, K; Iiai, T; Minagawa, M; Sato, Y; Yamamoto, S, 2005) | 0.33 |
| " Contrary to the known potential of repeated parenteral dosing with alpha-GalCer to induce NKT cell anergy that could compromise adoptive immunity development, we have observed that two and three doses delivered by the intranasal or oral route were more efficient in priming broader antigen-specific immune responses." | ( Alpha-galactosylceramide is an effective mucosal adjuvant for repeated intranasal or oral delivery of HIV peptide antigens. Courtney, AN; Nehete, BP; Nehete, PN; Sastry, KJ; Thapa, P; Zhou, D, 2009) | 0.35 |
| " We evaluated the delivery of the NKT cell ligand, α-galactosylceramide (α-GalCer), in 27 macaques by studying the effects of different dosing (1-100 μg), and delivery modes [directly intravenously (i." | ( In-vivo stimulation of macaque natural killer T cells with α-galactosylceramide. Fernandez, CS; Godfrey, DI; Jegaskanda, S; Kent, SJ, 2013) | 0.39 |
| " Here, we describe the potential of a novel approach using a ligand for iNKT cells and suboptimal dosage of antibody for CD40-CD40 ligand (L) blockade as a powerful method for mixed chimerism establishment after allogenic bone marrow transplantation in sublethally irradiated fully allo recipients." | ( A novel approach inducing transplant tolerance by activated invariant natural killer T cells with costimulatory blockade. Fukuda, E; Hirai, T; Ikemiyagi, M; Ishii, Y; Namiki, M; Omoto, K; Tanabe, K; Taniguchi, M, 2014) | 0.4 |
| " A multiple dosing regimen reduced tumor burden and prolonged the life of mice, whereas tumors returned within 5 days after a single dose of α-GalCer." | ( Imaging α-GalCer-Activated iNKT Cells in a Hepatic Metastatic Environment. Babes, L; Kubes, P; Shim, R, 2022) | 0.72 |
| Role | Description |
|---|---|
| antineoplastic agent | A substance that inhibits or prevents the proliferation of neoplasms. |
| epitope | The biological role played by a material entity when bound by a receptor of the adaptive immune system. Specific site on an antigen to which an antibody binds. |
| antigen | Any substance that stimulates an immune response in the body, such as through antibody production or by presentation to a T-cell receptor after binding to a major histocompability complex (MHC). |
| immunological adjuvant | A substance that augments, stimulates, activates, potentiates, or modulates the immune response at either the cellular or humoral level. A classical agent (Freund's adjuvant, BCG, Corynebacterium parvum, et al.) contains bacterial antigens. It could also be endogenous (e.g., histamine, interferon, transfer factor, tuftsin, interleukin-1). Its mode of action is either non-specific, resulting in increased immune responsiveness to a wide variety of antigens, or antigen-specific, i.e., affecting a restricted type of immune response to a narrow group of antigens. The therapeutic efficacy is related to its antigen-specific immunoadjuvanticity. |
| allergen | A chemical compound, or part thereof, which causes the onset of an allergic reaction by interacting with any of the molecular pathways involved in an allergy. |
| [role information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Class | Description |
|---|---|
| glycophytoceramide | A phytoceramide having at least one glycosyl group attached to either of its hydroxy groups. |
| N-acyl-beta-D-galactosylphytosphingosine | |
| [compound class information is derived from Chemical Entities of Biological Interest (ChEBI), Hastings J, Owen G, Dekker A, Ennis M, Kale N, Muthukrishnan V, Turner S, Swainston N, Mendes P, Steinbeck C. (2016). ChEBI in 2016: Improved services and an expanding collection of metabolites. Nucleic Acids Res] | |
| Assay ID | Title | Year | Journal | Article |
|---|---|---|---|---|
| AID1650383 | Immunostimulatory activity in C57BL/6 mouse assessed as increase in IL-4 level in serum at 100 ug/kg, ip measured after 3 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis and biological activities of amino acids functionalized α-GalCer analogues. |
| AID593005 | Immunostimulatory activity in C57BL/6 mouse assessed as maximum INF-gamma level in serum at 10 ug/ml, iv after 2 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | Introduction of aromatic group on 4'-OH of α-GalCer manipulated NKT cell cytokine production. |
| AID674456 | Immunostimulatory activity in C57BL/6J mouse assessed as increase in IL4 level at 2 ug, iv by cytometric bead array method | 2012 | Bioorganic & medicinal chemistry, Jul-15, Volume: 20, Issue:14 | RCAI-84, 91, and 105-108, ureido and thioureido analogs of KRN7000: their synthesis and bioactivity for mouse lymphocytes to produce Th1-biased cytokines. |
| AID411353 | Induction of cytokine expression in C57BL/6 mouse iNKT cells at 100 ng/mL after 24 hrs by intracellular staining for IFN-gamma | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID295918 | Induction of IL4 secretion in C57BL/6 mouse spleen cells at 100 ng/ml after 72 hrs relative to OCH | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Minimum structure requirement of immunomodulatory glycolipids for predominant Th2 cytokine induction and the discovery of non-linear phytosphingosine analogs. |
| AID590445 | Induction of IFN-gamma production in BALB/c mouse after 6 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Use of the NEO strategy (Nucleophilic addition/Epoxide Opening) for the synthesis of a new C-galactoside ester analogue of KRN 7000. |
| AID1226748 | Immunostimulatory activity in B6 mouse assessed as induction of IL-4 production in serum at 100 ug/kg, ip measured at 3 hrs by ELISA | 2015 | ACS medicinal chemistry letters, Apr-09, Volume: 6, Issue:4 | Synthesis and Biological Activities of 5-Thio-α-GalCers. |
| AID327296 | Induction of IL10 secretion in BALB/c mouse serum at 2 ug, iv after 18 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID340068 | Induction of proliferation in mouse iNKT cells | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of all stereoisomers of KRN7000, the CD1d-binding NKT cell ligand. |
| AID411362 | Activation of iNKT cells in C57BL/6 mouse assessed as cell frequency at 5 or 10 ug, ip by FACS analysis | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID760648 | Immunostimulatory activity in C57BL/6J mouse assessed as increase in production of IL-4 in serum at 0.02 to 2 ug, iv measured at 3 hrs by cytometric bead array method | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | RCAI-61 and related 6'-modified analogs of KRN7000: their synthesis and bioactivity for mouse lymphocytes to produce interferon-γ in vivo. |
| AID327275 | Activation of dendritic cells in BALB/c mouse at 2 ug, iv after 72 hrs by flow cytometry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID421559 | Effect on immune response in human iNKT cells stimulated by antigen-presenting CD1d-transfected human HeLa cells assessed as induction of TNFalpha release by MTT assay | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000. |
| AID340072 | Induction of IFN-gamma production in human iNKT cells | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of all stereoisomers of KRN7000, the CD1d-binding NKT cell ligand. |
| AID421566 | Regulation of immune response in C57BL/6J mouse assessed as induction of NKT cell cytokine response-related IL2 secretion at 10 to 1000 ug/kg, ip after 2 hrs by ELISA | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000. |
| AID1567111 | Binding affinity to human CD1d expressed in human HeLa cells assessed as increase in IL-13 production at 10 uM to 10'-4 uM incubated overnight prior to iNKT MAD11 cells addition to CD1d-compound mixture and measured after 24 hrs by ELISA | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | 3,4-Dideoxy-3,3,4,4-tetrafluoro- and 4-OH epimeric 3-deoxy-3,3-difluoro-α-GalCer analogues: Synthesis and biological evaluation on human iNKT cells stimulation. |
| AID772497 | Immunomodulatory activity in PMA- and ionomycin-stimulated wild type C57BL/6 mouse HMNC cells assessed as reduction in IL-17 cytokine in cell culture supernatant at 2 ug, ip administered as single dose measured 22 days post immunization by ELISA relative | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Synthesis and biological evaluation of α-galactosylceramide analogues with heteroaromatic rings and varying positions of a phenyl group in the sphingosine backbone. |
| AID327254 | Induction of IL8 secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID551859 | Binding affinity to C1R-hCD1d expressed in human B cells assessed as activation of IL-4 release in human iNKT cells upto 100 ng/ml after 36 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis of truncated analogues of the iNKT cell agonist, α-galactosyl ceramide (KRN7000), and their biological evaluation. |
| AID277788 | Stimulation of IFN-gamma secretion from C57BL/6 mouse splenocytes at 125 ng/mL after 72 hrs | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3 | Synthesis and evaluation of 1,2,3-triazole containing analogues of the immunostimulant alpha-GalCer. |
| AID421569 | Regulation of immune response in C57BL/6J mouse assessed as induction of NKT cell cytokine response-related TNFalpha secretion at 100 ug/kg, ip after 4 hrs by ELISA | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000. |
| AID327297 | Induction of IL13 secretion in BALB/c mouse serum at 2 ug, iv after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID428461 | Immunostimulatory activity in iNKT hybridoma 1.2 cells expressing TCR Vbeta8.2 assessed as IL2 level by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and evaluation of 3''- and 4''-deoxy and -fluoro analogs of the immunostimulatory glycolipid, KRN7000. |
| AID327256 | Induction of IL3 secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID1593614 | Induction of serum IFNgamma production in C57BL/6 mouse assessed as serum IFNgamma level at 100 ug/kg, ip and measured for 48 hrs by AUC method | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Design, synthesis, and evaluation of α-galactopyranosylceramide mimics promoting Th2 cytokines production. |
| AID327281 | Antitumor activity in mouse 4T1 cells xenografted BALB/c mouse assessed as suppression of tumor growth at 2 ug, iv | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID292516 | Binding affinity to T cell receptor | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15 | Modification of the ceramide moiety of isoglobotrihexosylceramide on its agonist activity in stimulation of invariant natural killer T cells. |
| AID327291 | Induction of TNFalpha secretion in BALB/c mouse serum at 2 ug, iv after 18 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID110022 | Tumor Growth Inhibitory effect (TGIR) on mice subcutaneously inoculated with B16 cells (compound plus MMC) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID92413 | Lymphocyte Proliferation Stimulatory effect on human umbilical cord blood at 100 ng/mL and measured for [3H]TdR (tritium-thymidine) uptake (percent of control) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID140769 | Lymphocyte Proliferation Stimulatory effect on Allogenic MLR at 0.1 ng/mL and measured for [3H]TdR (tritium-thymidine) uptake (percent of control) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID1226749 | Immunostimulatory activity in B6 mouse assessed as induction of IFN-gamma production in serum at 100 ug/kg, ip measured at 6 to 24 hrs by ELISA | 2015 | ACS medicinal chemistry letters, Apr-09, Volume: 6, Issue:4 | Synthesis and Biological Activities of 5-Thio-α-GalCers. |
| AID387827 | Induction of IL13 production in C57BL/6 mouse natural killer T cells after 48 hrs by cytometric bead array | 2008 | Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19 | RCAI-17, 22, 24-26, 29, 31, 34-36, 38-40, and 88, the analogs of KRN7000 with a sulfonamide linkage: their synthesis and bioactivity for mouse natural killer T cells to produce Th2-biased cytokines. |
| AID590444 | Induction of IL-4 production in BALB/c mouse after 6 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Use of the NEO strategy (Nucleophilic addition/Epoxide Opening) for the synthesis of a new C-galactoside ester analogue of KRN 7000. |
| AID1296718 | Binding affinity to CD1D in Balb/c mouse splenocytes assessed as increase in IL-2 production at 10 to 1000 ng/ml after 48 hrs by sandwich ELISA | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues. |
| AID1296717 | Binding affinity to CD1D in Balb/c mouse splenocytes assessed as increase in IL-4 production at 10 to 1000 ng/ml after 48 hrs by sandwich ELISA | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues. |
| AID432524 | Activation of mouse DN32 cells co-cultured with CD1d-transfected RAW cells assessed as IL-2 release at 100 ng/ml fixed and then pulsed for 3 hrs measured after 16 hrs by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and biological activity of alpha-galactosyl ceramide KRN7000 and galactosyl (alpha1-->2) galactosyl ceramide. |
| AID1650392 | Binding affinity to CD1d in C57BL/6 mouse splenocytes assessed as iNKT cell stimulating activity by measuring maximal induction of Th2-cytokine, IL-4 production at 1 uM incubated for 48 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis and biological activities of amino acids functionalized α-GalCer analogues. |
| AID1137769 | Stimulation of mouse CD1d-mediated IFN-gamma production in C57BL/6 mouse splenocytes measured at 32 ng/ml after 72 hrs by ELISA | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Design and Evaluation of ω-Hydroxy Fatty Acids Containing α-GalCer Analogues for CD1d-Mediated NKT Cell Activation. |
| AID772496 | Immunomodulatory activity in PMA- and ionomycin-stimulated wild type C57BL/6 mouse HMNC cells assessed as reduction in IFN-gamma cytokine in cell culture supernatant at 2 ug, ip administered as single dose measured 22 days post immunization by ELISA relat | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Synthesis and biological evaluation of α-galactosylceramide analogues with heteroaromatic rings and varying positions of a phenyl group in the sphingosine backbone. |
| AID1593618 | Ratio of induction activity for IL-4 production in C57BL/6 mouse at 100 ug/kg, ip after 48 hrs by AUC method to induction activity for IFN-gamma production in C57BL/6 mouse at 100 ug/kg, ip after 48 hrs by AUC method | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Design, synthesis, and evaluation of α-galactopyranosylceramide mimics promoting Th2 cytokines production. |
| AID593002 | Immunostimulatory activity in C57BL/6 mouse assessed as IL4 level in serum at 10 ug/ml, iv after 2 to 24 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | Introduction of aromatic group on 4'-OH of α-GalCer manipulated NKT cell cytokine production. |
| AID89015 | Lymphocyte Proliferation Stimulatory effect on human peripheral blood at 10 ng/mL and measured for [3H]TdR (tritium-thymidine) uptake (percent of control) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID411366 | Induction of cytokine expression in NOD mouse iNKT cells at 200 ng/mL after 24 hrs by intracellular staining for IFN-gamma | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID277791 | Elevation of IFN-gamma in C57B/6 mouse at 1 ug, iv after 12 hrs | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3 | Synthesis and evaluation of 1,2,3-triazole containing analogues of the immunostimulant alpha-GalCer. |
| AID327248 | Induction of IL2 secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID1567110 | Binding affinity to human CD1d expressed in human HeLa cells assessed as increase in IFNgamma production at 10 uM to 10'-4 uM incubated overnight prior to iNKT MAD11 cells addition to CD1d-compound mixture and measured after 6 hrs by ELISA | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | 3,4-Dideoxy-3,3,4,4-tetrafluoro- and 4-OH epimeric 3-deoxy-3,3-difluoro-α-GalCer analogues: Synthesis and biological evaluation on human iNKT cells stimulation. |
| AID327251 | Induction of RANTES secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID327295 | Induction of IL6 secretion in BALB/c mouse serum at 2 ug, iv after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID327247 | Induction of IFN-gamma secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID661317 | Activation of Namalwa cell expressing CD1D-TCR in human MAD11 cells assessed as TH1-mediated TNFalpha secretion after 6 hrs relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | 3-fluoro- and 3,3-difluoro-3,4-dideoxy-KRN7000 analogues as new potent immunostimulator agents: total synthesis and biological evaluation in human invariant natural killer T cells and mice. |
| AID327274 | Activation of TCR in human immature dendritic cells assessed as increase in CREB phosphorylation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID110021 | Tumor Growth Inhibitory effect (TGIR) on mice subcutaneously inoculated with B16 cells (compound alone (single)) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID421572 | Regulation of immune response in C57BL/6J mouse assessed as induction of NKT cell cytokine response-related IL4 secretion at 100 ug/kg, ip after 4 hrs by ELISA | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000. |
| AID327261 | Induction of IL10 secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID551860 | Binding affinity to C1R-hCD1d expressed in human B cells assessed as change in IFN-gamma/IL4 ratio in human iNKT cells upto 100 ng/ml after 36 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis of truncated analogues of the iNKT cell agonist, α-galactosyl ceramide (KRN7000), and their biological evaluation. |
| AID327257 | Induction of GM-CSF secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID327255 | Induction of TNFalpha secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID551856 | Binding affinity to C1R-hCD1d expressed in human B cells assessed as increase in Th1 cytokine release in mouse iNKT cells upto 100 ng/ml after 36 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis of truncated analogues of the iNKT cell agonist, α-galactosyl ceramide (KRN7000), and their biological evaluation. |
| AID1598834 | Stimulation of cytokine secretion in C57BL/6 mouse HMNCs assessed as increase in IL-4 secretion at 25 nM measured after 72 hrs by ELISA | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Improved Th17 Selectivity of α-Galactosylceramide via Noncovalent Interactions with Diether Moiety. |
| AID432520 | Activation of human BM2a.3 cells co-cultured with CD1d-expressing U937 cells assessed as IFN-gamma release after 16 hrs by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and biological activity of alpha-galactosyl ceramide KRN7000 and galactosyl (alpha1-->2) galactosyl ceramide. |
| AID411359 | Induction of cell proliferation in C57BL/6 mouse iNKT cells at 200 ng/mL after 24 hrs by CFSE dilution | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID1537552 | Immunomodulatory activity in C57BL/6 mouse assessed as serum IFNgamma/IL-4 maximum productivity ratio at 100 ug/kg, ip by ELISA | |||
| AID1454461 | Immunostimulatory activity in human iNKT cells cocultured with HeLa CD1d cells assessed as induction of IFNgamma levels at 0.01 to 1 nM after 24 hrs by ELISA | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6 | Efficient Divergent Synthesis of New Immunostimulant 4″-Modified α-Galactosylceramide Analogues. |
| AID1509401 | Binding affinity to CD1d in C57BL/6 mouse HMNC cells assessed as iNKT cells stimulation by measuring increase in IL-2 production at 25 nM incubated for 72 hrs by ELISA | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Development of α-GalCer Analogues with an α-Fluorocarbonyl Moiety as Th2-Selective Ligands of CD1d. |
| AID677315 | Immunostimulatory activity in C57BL/6 mouse splenocytes assessed as IL-4 release at 100 ng/ml after 72 hrs by ELISA relative to OCH | 2012 | Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9 | Synthesis and biological evaluation of truncated α-galactosylceramide derivatives focusing on cytokine induction profile. |
| AID327279 | Increase in CD8/CD4 T cell ratio in BALB/c mouse at 2 ug, iv after 72 hrs by flow cytometry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID421563 | Effect on immune response in human iNKT cells stimulated by antigen-presenting CD1d-transfected human HeLa cells assessed as induction of IL4 release by ELISA | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000. |
| AID327272 | Activation of TCR in human immature dendritic cells assessed as increase in ERK1/2 phosphorylation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID1454460 | Immunostimulatory activity in C57BL/6 mouse assessed as induction of IL-4 levels in serum at 2.0 x 10'-4 ug/kg, ip measured after 4 hrs by ELISA | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6 | Efficient Divergent Synthesis of New Immunostimulant 4″-Modified α-Galactosylceramide Analogues. |
| AID421562 | Effect on immune response in human iNKT cells stimulated by antigen-presenting CD1d-transfected human HeLa cells assessed as induction of IFN-gamma release by ELISA | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000. |
| AID1537553 | Immunomodulatory activity in C57BL/6 mouse assessed as serum IFNgamma/IL-4 AUC ratio at 100 ug/kg, ip by ELISA | |||
| AID411369 | Induction of cell proliferation in NOD mouse iNKT cells at 100 ng/mL after 48 hrs by CFSE dilution | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID327287 | Induction of RANTES secretion in BALB/c mouse serum at 2 ug, iv after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID277792 | Stimulation of IL4 secretion from C57BL/6 mouse splenocytes at 125 ng/mL after 72 hrs | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3 | Synthesis and evaluation of 1,2,3-triazole containing analogues of the immunostimulant alpha-GalCer. |
| AID327294 | Induction of IL4 secretion in BALB/c mouse serum at 2 ug, iv after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID295919 | Induction of IFN gamma secretion in C57BL/6 mouse spleen cells at 100 ng/ml after 72 hrs relative to OCH | 2007 | Bioorganic & medicinal chemistry letters, May-15, Volume: 17, Issue:10 | Minimum structure requirement of immunomodulatory glycolipids for predominant Th2 cytokine induction and the discovery of non-linear phytosphingosine analogs. |
| AID421558 | Regulation of immune response in C57BL/6J mouse assessed as induction of NKT cell cytokine response-related IFN-gamma secretion at 100 ug/kg, ip after 18 hrs by ELISA | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000. |
| AID458489 | Induction of CD1D-mediated IL-13 production in human iNKT cells expressing CD4 at 400 nM after 18 hrs by ELISA | 2010 | Bioorganic & medicinal chemistry letters, Feb-01, Volume: 20, Issue:3 | Syntheses and biological activities of KRN7000 analogues having aromatic residues in the acyl and backbone chains with varying stereochemistry. |
| AID671522 | Immunomodulatory activity in mouse hepatic mononuclear cells containing iNKT cells assessed as IFNgamma release at 25 nM after 72 hrs by ELISA | 2012 | ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2 | Heteroaromatic Moieties in the Sphingosine Backbone of α-Galactosylceramides for Noncovalent Interactions with CD1d. |
| AID575776 | Antibacterial activity against Sphingomonas capsulata ATCC 14666 infected in C57BL/6 mouse assessed as reduction in lung bacterial load at 100 ug/kg, ip administered 2 hrs post infection measured 24 hrs post infection | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10 | In vivo protection provided by a synthetic new alpha-galactosyl ceramide analog against bacterial and viral infections in murine models. |
| AID1666607 | Binding affinity to CD1d in Traj18 knock out C57BL/6 mouse assessed as restriction ratio for reduction in iNKT/CD1d interaction by FACS analysis relative to control | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Photo effect on the CD1d-binding ability of azobenzene-attached analogues of α-GalCer. |
| AID327290 | Induction of KC secretion in BALB/c mouse serum at 2 ug, iv after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID1650384 | Immunostimulatory activity in C57BL/6 mouse assessed as increase in IFN-gamma level in serum at 100 ug/kg, ip measured after 6 to 24 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis and biological activities of amino acids functionalized α-GalCer analogues. |
| AID340074 | Induction of IL13 production in human iNKT cells | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of all stereoisomers of KRN7000, the CD1d-binding NKT cell ligand. |
| AID411367 | Induction of cytokine expression in NOD mouse iNKT cells at 200 ng/mL after 48 hrs by intracellular staining for IFN-gamma | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID1650386 | Immunostimulatory activity in C57BL/6 mouse assessed as IFN-gamma level in serum at 100 ug/kg, ip measured after 24 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis and biological activities of amino acids functionalized α-GalCer analogues. |
| AID340073 | Induction of IL4 production in human iNKT cells | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of all stereoisomers of KRN7000, the CD1d-binding NKT cell ligand. |
| AID1137770 | In vivo stimulation of mouse CD1d-mediated peak IL4 production in C57BL/6 mouse serum measured at 0.5 ug, iv after 2 hrs by ELISA | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Design and Evaluation of ω-Hydroxy Fatty Acids Containing α-GalCer Analogues for CD1d-Mediated NKT Cell Activation. |
| AID661324 | Activation of Namalwa cell expressing CD1D-TCR in human MAD11 cells assessed as TH1-mediated IFN-gamma secretion after 6 hrs by ELISA relative to KRN7000 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | 3-fluoro- and 3,3-difluoro-3,4-dideoxy-KRN7000 analogues as new potent immunostimulator agents: total synthesis and biological evaluation in human invariant natural killer T cells and mice. |
| AID142473 | [3H]TdR uptake measured by spleen cell proliferation assay by adding compound dose of 100 ng/mL | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10 | Syntheses of biotinylated alpha-galactosylceramides and their effects on the immune system and CD1 molecules. |
| AID327293 | Induction of GM-CSF secretion in BALB/c mouse serum at 2 ug, iv after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID142472 | [3H]TdR uptake measured by spleen cell proliferation assay by adding compound dose of 10 ng/mL | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10 | Syntheses of biotinylated alpha-galactosylceramides and their effects on the immune system and CD1 molecules. |
| AID411363 | Activation of iNKT cells in NOD mouse assessed as cell frequency at 5 or 10 ug, ip by FACS analysis | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID327270 | Activation of TCR in human immature dendritic cells assessed as increase in CD3epsilon phosphorylation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID551858 | Binding affinity to C1R-hCD1d expressed in human B cells assessed as activation of IFN-gamma release in human iNKT cells upto 100 ng/ml after 36 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis of truncated analogues of the iNKT cell agonist, α-galactosyl ceramide (KRN7000), and their biological evaluation. |
| AID327280 | Antitumor activity in TC1 cells xenografted C57BL/6 mouse assessed as suppression of tumor growth at 2 ug, iv | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID327286 | Induction of IL12p40 secretion in BALB/c mouse serum at 2 ug, iv after 18 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID671523 | Immunomodulatory activity in mouse hepatic mononuclear cells containing iNKT cells assessed as IL4 release at 25 nM after 72 hrs by ELISA | 2012 | ACS medicinal chemistry letters, Feb-09, Volume: 3, Issue:2 | Heteroaromatic Moieties in the Sphingosine Backbone of α-Galactosylceramides for Noncovalent Interactions with CD1d. |
| AID1666606 | Binding affinity to WTB6 mouse spleen CD1d assessed as restriction ratio for reduction in iNKT/CD1d interaction by FACS analysis relative to control | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Photo effect on the CD1d-binding ability of azobenzene-attached analogues of α-GalCer. |
| AID1137771 | In vivo stimulation of mouse CD1d-mediated peak IFN-gamma production in C57BL/6 mouse serum measured at 0.5 ug, iv after 12 hrs by ELISA | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Design and Evaluation of ω-Hydroxy Fatty Acids Containing α-GalCer Analogues for CD1d-Mediated NKT Cell Activation. |
| AID92299 | Lymphocyte Proliferation Stimulatory effect on human umbilical cord blood at 10 ng/mL and measured for [3H]TdR (tritium-thymidine) uptake (percent of control) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID1666605 | Binding affinity to WTB6 mouse thymus CD1d assessed as restriction ratio for reduction in iNKT/CD1d interaction by FACS analysis relative to control | 2020 | Bioorganic & medicinal chemistry letters, 03-01, Volume: 30, Issue:5 | Photo effect on the CD1d-binding ability of azobenzene-attached analogues of α-GalCer. |
| AID483197 | Induction of cellular expansion in human iNKT cells at 250 nM after 8 days | 2010 | Bioorganic & medicinal chemistry letters, Jun-15, Volume: 20, Issue:12 | Synthesis and biological activity of alpha-glucosyl C24:0 and C20:2 ceramides. |
| AID387826 | Induction of IL4 production in C57BL/6 mouse natural killer T cells after 48 hrs by cytometric bead array | 2008 | Bioorganic & medicinal chemistry, Oct-01, Volume: 16, Issue:19 | RCAI-17, 22, 24-26, 29, 31, 34-36, 38-40, and 88, the analogs of KRN7000 with a sulfonamide linkage: their synthesis and bioactivity for mouse natural killer T cells to produce Th2-biased cytokines. |
| AID661318 | Activation of Hela cell expressing human CD1D-TCR in human MAD11 cells assessed as TH1-mediated IFN-gamma secretion after 6 hrs by ELISA relative to KRN7000 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | 3-fluoro- and 3,3-difluoro-3,4-dideoxy-KRN7000 analogues as new potent immunostimulator agents: total synthesis and biological evaluation in human invariant natural killer T cells and mice. |
| AID432521 | Activation of mouse DN32 cells in co-cultured with CD1d-transfected RAW cells assessed as IL-2 release after 16 hrs by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and biological activity of alpha-galactosyl ceramide KRN7000 and galactosyl (alpha1-->2) galactosyl ceramide. |
| AID772498 | Immunomodulatory activity in PMA- and ionomycin-stimulated wild type C57BL/6 mouse HMNC cells assessed as inhibition of Th17 differentiation of MOG-specific CD4+ T cells at 2 ug, ip administered as single dose measured 22 days post immunization by brefeld | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Synthesis and biological evaluation of α-galactosylceramide analogues with heteroaromatic rings and varying positions of a phenyl group in the sphingosine backbone. |
| AID421565 | Regulation of immune response in C57BL/6J mouse assessed as induction of NKT cell cytokine response-related IFN-gamma secretion at 10 to 1000 ug/kg, ip after 14 hrs by ELISA | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000. |
| AID1567112 | Effect on human iNKT MAD11 cells stimulation assessed as increase in IFNgamma production pretreated with HeLa cells for overnight prior to iNKT MAD11 cells addition and measured after 6 hrs by ELISA | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | 3,4-Dideoxy-3,3,4,4-tetrafluoro- and 4-OH epimeric 3-deoxy-3,3-difluoro-α-GalCer analogues: Synthesis and biological evaluation on human iNKT cells stimulation. |
| AID327250 | Induction of IL12p40 secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID142471 | [3H]-TdR uptake measured by spleen cell proliferation assay by adding compound dose of 1 ng/mL | 1999 | Journal of medicinal chemistry, May-20, Volume: 42, Issue:10 | Syntheses of biotinylated alpha-galactosylceramides and their effects on the immune system and CD1 molecules. |
| AID1296716 | Cytotoxicity against Balb/c mouse splenocytes assessed as reduction in cell proliferation up to 1000 ng/ml after 48 hrs by MTT assay | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues. |
| AID277790 | Elevation of IL4 in C57B/6 mouse at 1 ug, iv after 2 hrs | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3 | Synthesis and evaluation of 1,2,3-triazole containing analogues of the immunostimulant alpha-GalCer. |
| AID327271 | Activation of TCR in human HeLa cells overexpressing CD1d assessed as increase in ERK1/2 phosphorylation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID1306876 | Activity at CD1d in C57BL/6 mouse splenocytes assessed as production of IL4 at 10 to 1000 nM after 48 hrs by ELISA | 2016 | Bioorganic & medicinal chemistry, 08-15, Volume: 24, Issue:16 | Synthesis and Th1-immunostimulatory activity of α-galactosylceramide analogues bearing a halogen-containing or selenium-containing acyl chain. |
| AID1296719 | Binding affinity to CD1D in Balb/c mouse splenocytes assessed as increase in IFN-gamma production at 10 to 1000 ng/ml after 48 hrs by sandwich ELISA | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues. |
| AID340070 | Induction of IL4/IL13 production in mouse iNKT cells | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of all stereoisomers of KRN7000, the CD1d-binding NKT cell ligand. |
| AID327283 | Induction of IL1-beta secretion in BALB/c mouse serum at 2 ug, iv after 18 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID1296725 | Binding affinity to CD1D (unknown origin) assessed as increase in IL-2 production at 100 ng/ml preincubated for 16 hrs followed by Valpha-14 Vbeta-8.2 DN3A4-1.2(1.2) iNKT hybridoma cells addition to compound-CD1D mixture measured after 16 hrs by sandwich | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues. |
| AID292515 | Stimulation of hCD1d-restricted human iNKT cells assessed as IL4 release at 10 ng/mL by ELISA | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15 | Modification of the ceramide moiety of isoglobotrihexosylceramide on its agonist activity in stimulation of invariant natural killer T cells. |
| AID89016 | Lymphocyte Proliferation Stimulatory effect on human peripheral blood at 100 ng/mL and measured for [3H]TdR (tritium-thymidine) uptake (percent of control) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID1296722 | Binding affinity to CD1D in Balb/c mouse splenocytes assessed as increase in IL-4 production at 1000 ng/ml up to 24 hrs by sandwich ELISA | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues. |
| AID327260 | Induction of IL6 secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID292514 | Stimulation of hCD1d-restricted human iNKT cells assessed as IFN-gamma release at 10 ng/mL by ELISA | 2007 | Journal of medicinal chemistry, Jul-26, Volume: 50, Issue:15 | Modification of the ceramide moiety of isoglobotrihexosylceramide on its agonist activity in stimulation of invariant natural killer T cells. |
| AID327284 | Induction of IL2 secretion in BALB/c mouse serum at 2 ug, iv after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID1593615 | Induction of serum IL-4 production in C57BL/6 mouse assessed as serum IL-4 level at 100 ug/kg, ip and measured for 48 hrs by AUC method | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Design, synthesis, and evaluation of α-galactopyranosylceramide mimics promoting Th2 cytokines production. |
| AID411371 | Induction of cell proliferation in NOD mouse iNKT cells at 200 ng/mL after 48 hrs by CFSE dilution | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID1296728 | Stimulation of IL-4 production in Balb/c mouse at 1 ug, iv after 2 to 48 hrs by sandwich ELISA | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues. |
| AID1137767 | Stimulation of mouse CD1d-mediated IL-2 production in DN32.D3 hybridoma cells co-cultured with mouse CD1d transfected RBL cells measured at 32 to 500 ng/ml after 4 hrs by ELISA | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Design and Evaluation of ω-Hydroxy Fatty Acids Containing α-GalCer Analogues for CD1d-Mediated NKT Cell Activation. |
| AID772503 | Invivo immunomodulatory activity in wild type C57BL/6 mouse assessed as IL-4 level in serum at 2 ug, iv administered as single dose measured at >2 hrs | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Synthesis and biological evaluation of α-galactosylceramide analogues with heteroaromatic rings and varying positions of a phenyl group in the sphingosine backbone. |
| AID551861 | Binding affinity to C1R-hCD1d expressed in human B cells assessed as increase in IFN-gamma/IL4 ratio in mouse iNKT cells upto 100 ng/ml after 36 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry, Jan-01, Volume: 19, Issue:1 | Synthesis of truncated analogues of the iNKT cell agonist, α-galactosyl ceramide (KRN7000), and their biological evaluation. |
| AID1296723 | Binding affinity to CD1D in Balb/c mouse splenocytes assessed as increase in IFN-gamma production at 1000 ng/ml up to 12 hrs by sandwich ELISA | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues. |
| AID327269 | Activation of TCR in human HeLa cells overexpressing CD1d assessed as increase in CD3epsilon phosphorylation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID327288 | Induction of MIPbeta secretion in BALB/c mouse serum at 2 ug, iv after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID340069 | Induction of IFN-gamma production in mouse iNKT cells | 2008 | Bioorganic & medicinal chemistry letters, Jul-15, Volume: 18, Issue:14 | Synthesis of all stereoisomers of KRN7000, the CD1d-binding NKT cell ligand. |
| AID592908 | Immunostimulatory activity in mouse DN3A4-1.2 cells expressing TCR assessed as IL2 level after 24 hrs by ELISA in presence of mouse CD1d protein | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | Introduction of aromatic group on 4'-OH of α-GalCer manipulated NKT cell cytokine production. |
| AID411352 | Activation of iNKT cells in C57BL/6 mouse assessed as intracellular cytokine expression at 5 or 10 ug, ip by FACS analysis | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID1296727 | Stimulation of IFN-gamma production in Balb/c mouse at 1 ug, iv after 2 to 48 hrs by sandwich ELISA | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues. |
| AID327292 | Induction of IL3 secretion in BALB/c mouse serum at 2 ug, iv after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID677316 | Immunostimulatory activity in C57BL/6 mouse splenocytes assessed as IFN-gamma release at 100 ng/ml after 72 hrs by ELISA relative to OCH | 2012 | Bioorganic & medicinal chemistry, May-01, Volume: 20, Issue:9 | Synthesis and biological evaluation of truncated α-galactosylceramide derivatives focusing on cytokine induction profile. |
| AID432522 | Activation of mouse DN32 cells in co-cultured with plate bound antigen presenting cell free CD1d-FC fusion protein assessed as IL-2 release after 16 hrs by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and biological activity of alpha-galactosyl ceramide KRN7000 and galactosyl (alpha1-->2) galactosyl ceramide. |
| AID110020 | Tumor Growth Inhibitory effect (TGIR) on mice subcutaneously inoculated with B16 cells (chemotherapeutic agent, mitomycin C (MMC)) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID1226754 | Immunostimulatory activity in B6 mouse iNKT cells assessed as induction of IFN-gamma production at 1000 ng/ml incubated for 16 hrs followed by brefeldin A addition measured after 2 hrs by flow cytometric analysis (Rvb = 0.6%) | 2015 | ACS medicinal chemistry letters, Apr-09, Volume: 6, Issue:4 | Synthesis and Biological Activities of 5-Thio-α-GalCers. |
| AID327263 | Stimulation of cell expansion of human invariant CD161+/ Valpha24+/ CD56+/ CD3+ NKT cells by flow cytometry method | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID661316 | Activation of Hela cell expressing human CD1D-TCR in human MAD11 cells assessed as TH1-mediated TNFalpha secretion after 6 hrs relative to control | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | 3-fluoro- and 3,3-difluoro-3,4-dideoxy-KRN7000 analogues as new potent immunostimulator agents: total synthesis and biological evaluation in human invariant natural killer T cells and mice. |
| AID1593621 | Induction of serum IFNgamma production in C57BL/6 mouse assessed as serum IFNgamma level at 100 ug/kg, ip and measured for 48 hrs by peak value method | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Design, synthesis, and evaluation of α-galactopyranosylceramide mimics promoting Th2 cytokines production. |
| AID1509402 | Binding affinity to CD1d in C57BL/6 mouse HMNC cells assessed as iNKT cells stimulation by measuring increase in Th2-type cytokine, IL-4 production at 25 nM incubated for 72 hrs by ELISA | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Development of α-GalCer Analogues with an α-Fluorocarbonyl Moiety as Th2-Selective Ligands of CD1d. |
| AID428462 | Immunostimulatory activity in iNKT hybridoma 2H4 cells expressing TCR Vbeta7 assessed as IL2 level by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and evaluation of 3''- and 4''-deoxy and -fluoro analogs of the immunostimulatory glycolipid, KRN7000. |
| AID327258 | Induction of IL15 secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID1593619 | Induction of serum IL-4 production in C57BL/6 mouse assessed as serum IL-4 level at 100 ug/kg, ip and measured for 48 hrs by peak value method | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Design, synthesis, and evaluation of α-galactopyranosylceramide mimics promoting Th2 cytokines production. |
| AID1593623 | Ratio of induction activity for IL-4 production in C57BL/6 mouse at 100 ug/kg, ip after 48 hrs by peak value method to induction activity for IFN-gamma production in C57BL/6 mouse at 100 ug/kg, ip after 48 hrs by peak value method | 2019 | Bioorganic & medicinal chemistry letters, 06-01, Volume: 29, Issue:11 | Design, synthesis, and evaluation of α-galactopyranosylceramide mimics promoting Th2 cytokines production. |
| AID592997 | Immunostimulatory activity in mouse N38.2H4 cells expressing TCR assessed as IL2 level after 24 by ELISA in presence of mouse CD1d protein | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | Introduction of aromatic group on 4'-OH of α-GalCer manipulated NKT cell cytokine production. |
| AID411358 | Induction of cell proliferation in C57BL/6 mouse iNKT cells at 100 ng/mL after 48 hrs by CFSE dilution | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID411364 | Induction of cytokine expression in NOD mouse iNKT cells at 100 ng/mL after 24 hrs by intracellular staining for IFN-gamma | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID327285 | Induction of IL12p70 secretion in BALB/c mouse serum at 2 ug, iv after 18 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID327289 | Induction of MCP1 secretion in BALB/c mouse serum at 2 ug, iv after 2 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID327273 | Activation of TCR in human HeLa cells overexpressing CD1d assessed as increase in CREB phosphorylation | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID483709 | Effect on immune response in human iNKT cells stimulated by antigen-presenting CD1d assessed as cellular expansion at 250 nM after 8 days by FACSCalibur flow cytometry relative to control | 2010 | Bioorganic & medicinal chemistry letters, Jun-01, Volume: 20, Issue:11 | Synthesis and biological activity of alpha-L-fucosyl ceramides, analogues of the potent agonist, alpha-D-galactosyl ceramide KRN7000. |
| AID772499 | Immunomodulatory activity in PMA- and ionomycin-stimulated wild type C57BL/6 mouse HMNC cells assessed as inhibition of Th1 differentiation of MOG-specific CD4+ T cells at 2 ug, ip administered as single dose measured 22 days post immunization by brefeldi | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Synthesis and biological evaluation of α-galactosylceramide analogues with heteroaromatic rings and varying positions of a phenyl group in the sphingosine backbone. |
| AID1537549 | Immunomodulatory activity in C57BL/6 mouse assessed as increase in IL-4 secretion in serum at 100 ug/kg, ip after 3 hrs by ELISA | |||
| AID411354 | Induction of cytokine expression in C57BL/6 mouse iNKT cells at 100 ng/mL after 48 hrs by intracellular staining for IFN-gamma | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID327278 | Activation of B cells in BALB/c mouse at 2 ug, iv after 72 hrs by flow cytometry | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID661323 | Activation of Hela cell expressing human CD1D-TCR in human MAD11 cells assessed as TH2-mediated IL-13 secretion after 48 hrs by ELISA relative to KRN7000 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | 3-fluoro- and 3,3-difluoro-3,4-dideoxy-KRN7000 analogues as new potent immunostimulator agents: total synthesis and biological evaluation in human invariant natural killer T cells and mice. |
| AID593001 | Immunostimulatory activity in C57BL/6 mouse assessed as INF-gamma level in serum at 10 ug/ml, iv after 2 to 24 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | Introduction of aromatic group on 4'-OH of α-GalCer manipulated NKT cell cytokine production. |
| AID92298 | Lymphocyte Proliferation Stimulatory effect on human umbilical cord blood at 1 ng/mL and measured for [3H]TdR (tritium-thymidine) uptake (percent of control) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID593004 | Immunostimulatory activity in C57BL/6 mouse assessed as maximum IL4 level in serum at 10 ug/ml, iv after 2 hrs by ELISA | 2011 | Bioorganic & medicinal chemistry, Apr-15, Volume: 19, Issue:8 | Introduction of aromatic group on 4'-OH of α-GalCer manipulated NKT cell cytokine production. |
| AID327252 | Induction of MIPalpha secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID1509404 | Binding affinity to CD1d in C57BL/6 mouse HMNC cells assessed as iNKT cells stimulation by measuring increase in IL17 production at 25 nM incubated for 72 hrs by ELISA | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Development of α-GalCer Analogues with an α-Fluorocarbonyl Moiety as Th2-Selective Ligands of CD1d. |
| AID1296724 | Binding affinity to CD1D in Balb/c mouse splenocytes assessed as increase in IFN-gamma production at 1000 ng/ml at 24 hrs by sandwich ELISA | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues. |
| AID277789 | Stimulation of IFN-gamma secretion from C57BL/6 mouse splenocytes at 32 ng/mL after 72 hrs | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3 | Synthesis and evaluation of 1,2,3-triazole containing analogues of the immunostimulant alpha-GalCer. |
| AID1650388 | Immunostimulatory activity in C57BL/6 mouse assessed as induction of Th1 cytokine-biased response by measuring AUC ratio of IFN-gamma/IL-4 cytokine release at 100 ug/kg, ip measured after 24 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis and biological activities of amino acids functionalized α-GalCer analogues. |
| AID140773 | Lymphocyte Proliferation Stimulatory effect on Allogenic MLR at 100 ng/mL and measured for [3H]-TdR (tritium-thymidine) uptake (percent of control) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID772495 | Antiautoimmune disease activity in wild type C57BL/6 mouse experimental autoimmune encephalitis model assessed as reduction in disease pathogenicity at 2 ug, ip administered as single dose measured up to 30 days | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Synthesis and biological evaluation of α-galactosylceramide analogues with heteroaromatic rings and varying positions of a phenyl group in the sphingosine backbone. |
| AID327249 | Induction of IL12p70 secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID411360 | Induction of cell proliferation in C57BL/6 mouse iNKT cells at 200 ng/mL after 48 hrs by CFSE dilution | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID1296721 | Binding affinity to CD1D in Balb/c mouse splenocytes assessed as increase in IL-4 production at 1000 ng/ml at 2 hrs by sandwich ELISA | 2016 | ACS medicinal chemistry letters, Feb-11, Volume: 7, Issue:2 | Design, Synthesis, and Immunological Evaluation of Benzyloxyalkyl-Substituted 1,2,3-Triazolyl α-GalCer Analogues. |
| AID590446 | Ratio of induction of IFN-gamma production to induction of IL-4 production in in BALB/c mouse after 6 hrs | 2011 | Bioorganic & medicinal chemistry letters, Apr-15, Volume: 21, Issue:8 | Use of the NEO strategy (Nucleophilic addition/Epoxide Opening) for the synthesis of a new C-galactoside ester analogue of KRN 7000. |
| AID140772 | Lymphocyte Proliferation Stimulatory effect on Allogenic MLR at 10 ng/mL and measured for [3H]TdR (tritium-thymidine) uptake (percent of control) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID411370 | Induction of cell proliferation in NOD mouse iNKT cells at 200 ng/mL after 24 hrs by CFSE dilution | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID1598837 | Stimulation of cytokine secretion in C57BL/6 mouse HMNCs assessed as increase in IFN gamma secretion at 25 nM measured after 72 hrs by ELISA | 2019 | ACS medicinal chemistry letters, May-09, Volume: 10, Issue:5 | Improved Th17 Selectivity of α-Galactosylceramide via Noncovalent Interactions with Diether Moiety. |
| AID432523 | Activation of mouse DN32 cells co-cultured with CD1d-transfected RAW cells assessed as IL-2 release at 100 ng/ml pulsed for 3 hrs and then fixed measured after 16 hrs by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and biological activity of alpha-galactosyl ceramide KRN7000 and galactosyl (alpha1-->2) galactosyl ceramide. |
| AID89014 | Lymphocyte Proliferation Stimulatory effect on human peripheral blood at 1 ng/mL and measured for [3H]TdR (tritium-thymidine) uptake (percent of control) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| AID1650381 | Binding affinity to CD1d in C57BL/6 mouse splenocytes assessed as iNKT cell stimulating activity by measuring induction of Th2-cytokine, IL-4 production incubated for 48 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis and biological activities of amino acids functionalized α-GalCer analogues. |
| AID1454459 | Immunostimulatory activity in C57BL/6 mouse assessed as induction of IFNgamma levels in serum at 2.0 x 10'-4 ug/kg, ip measured after 16 hrs by ELISA | 2017 | ACS medicinal chemistry letters, Jun-08, Volume: 8, Issue:6 | Efficient Divergent Synthesis of New Immunostimulant 4″-Modified α-Galactosylceramide Analogues. |
| AID1650391 | Binding affinity to CD1d in C57BL/6 mouse splenocytes assessed as iNKT cell stimulating activity by measuring maximal induction of Th1-cytokine, IFN-gamma production at 1 uM incubated for 48 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis and biological activities of amino acids functionalized α-GalCer analogues. |
| AID760650 | Immunostimulatory activity in C57BL/6J mouse assessed as increase in production of IL-12p70 in serum at 2 ug, iv measured at 3 to 6 hrs by cytometric bead array method | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | RCAI-61 and related 6'-modified analogs of KRN7000: their synthesis and bioactivity for mouse lymphocytes to produce interferon-γ in vivo. |
| AID421567 | Regulation of immune response in C57BL/6J mouse assessed as induction of NKT cell cytokine response-related IL2 secretion at 10 to 1000 ug/kg, ip after 14 hrs by ELISA | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000. |
| AID1137768 | Stimulation of mouse CD1d-mediated IL-4 production in mouse splenocytes measured at 32 ng/ml after 72 hrs by ELISA | 2014 | ACS medicinal chemistry letters, Apr-10, Volume: 5, Issue:4 | Design and Evaluation of ω-Hydroxy Fatty Acids Containing α-GalCer Analogues for CD1d-Mediated NKT Cell Activation. |
| AID760652 | Immunostimulatory activity in C57BL/6J mouse assessed as increase in production of IFNgamma in serum at 2 ug, iv by ELISA | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | RCAI-61 and related 6'-modified analogs of KRN7000: their synthesis and bioactivity for mouse lymphocytes to produce interferon-γ in vivo. |
| AID428463 | Immunostimulatory activity in iNKT hybridoma 1.4 cells expressing TCR Vbeta10 assessed as IL2 level by ELISA | 2009 | Bioorganic & medicinal chemistry letters, Aug-01, Volume: 19, Issue:15 | Synthesis and evaluation of 3''- and 4''-deoxy and -fluoro analogs of the immunostimulatory glycolipid, KRN7000. |
| AID1650387 | Immunostimulatory activity in C57BL/6 mouse assessed as induction of Th1 cytokine-biased response by measuring IFN-gamma/IL-6 ratio at 100 ug/kg, ip measured after 24 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis and biological activities of amino acids functionalized α-GalCer analogues. |
| AID1537550 | Immunomodulatory activity in C57BL/6 mouse assessed as increase in IFN-gamma secretion in serum at 100 ug/kg, ip by ELISA | |||
| AID671518 | Immunostimulatory activity in mouse splenocytes assessed as IFNgamma production at 8 ng/ml after 72 hrs by ELISA | 2011 | ACS medicinal chemistry letters, Jul-14, Volume: 2, Issue:7 | The 3-Deoxy Analogue of α-GalCer: Disclosing the Role of the 4-Hydroxyl Group for CD1d-Mediated NKT Cell Activation. |
| AID772501 | Antiautoimmune disease activity in wild type C57BL/6 mouse experimental autoimmune encephalitis model assessed as delay in disease onset at 2 ug, ip administered as single dose measured up to 30 days | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Synthesis and biological evaluation of α-galactosylceramide analogues with heteroaromatic rings and varying positions of a phenyl group in the sphingosine backbone. |
| AID772505 | Invivo immunomodulatory activity in wild type C57BL/6 mouse assessed as IL-4 level in serum at 2 ug, iv administered as single dose measured at 2 hrs | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Synthesis and biological evaluation of α-galactosylceramide analogues with heteroaromatic rings and varying positions of a phenyl group in the sphingosine backbone. |
| AID411355 | Induction of cytokine expression in C57BL/6 mouse iNKT cells at 200 ng/mL after 24 hrs by intracellular staining for IFN-gamma | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID327282 | Induction of IFN-gamma secretion in BALB/c mouse serum at 2 ug, iv after 18 hrs relative to control | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID671517 | Immunostimulatory activity in mouse DN32.D3 NKT hybridoma cells assessed as IL-2 production after 16 hrs by ELISA | 2011 | ACS medicinal chemistry letters, Jul-14, Volume: 2, Issue:7 | The 3-Deoxy Analogue of α-GalCer: Disclosing the Role of the 4-Hydroxyl Group for CD1d-Mediated NKT Cell Activation. |
| AID1567113 | Effect on human iNKT MAD11 cells stimulation assessed as increase in IL-13 production pretreated with HeLa cells for overnight prior to iNKT MAD11 cells addition and measured after 24 hrs by ELISA | 2019 | European journal of medicinal chemistry, Sep-15, Volume: 178 | 3,4-Dideoxy-3,3,4,4-tetrafluoro- and 4-OH epimeric 3-deoxy-3,3-difluoro-α-GalCer analogues: Synthesis and biological evaluation on human iNKT cells stimulation. |
| AID411357 | Induction of cell proliferation in C57BL/6 mouse iNKT cells at 100 ng/mL after 24 hrs by CFSE dilution | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID575778 | Antibacterial activity against luminescent Staphylococcus aureus Xen29 infected in BALB/c mouse deep thigh wound infection model assessed as reduction in bacterial load at 150 ug/kg, ip administered 3 hrs post infection by iVIS in-vivo imaging system | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10 | In vivo protection provided by a synthetic new alpha-galactosyl ceramide analog against bacterial and viral infections in murine models. |
| AID671519 | Immunostimulatory activity in mouse splenocytes assessed as IL4 production at 8 ng/ml after 72 hrs by ELISA | 2011 | ACS medicinal chemistry letters, Jul-14, Volume: 2, Issue:7 | The 3-Deoxy Analogue of α-GalCer: Disclosing the Role of the 4-Hydroxyl Group for CD1d-Mediated NKT Cell Activation. |
| AID575769 | Antiviral activity against Japanese encephalitis virus RP-9 infected in C57BL/6 mouse assessed as mouse survival rate at 1 ug, ip administered one day before and 1 day after viral infection measured after 25 days post infection relative to solvent treated | 2010 | Antimicrobial agents and chemotherapy, Oct, Volume: 54, Issue:10 | In vivo protection provided by a synthetic new alpha-galactosyl ceramide analog against bacterial and viral infections in murine models. |
| AID411356 | Induction of cytokine expression in C57BL/6 mouse iNKT cells at 200 ng/mL after 48 hrs by intracellular staining for IFN-gamma | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID411365 | Induction of cytokine expression in NOD mouse iNKT cells at 100 ng/mL after 48 hrs by intracellular staining for IFN-gamma | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID772504 | Invivo immunomodulatory activity in wild type C57BL/6 mouse assessed as decrease in IFN-gamma level in serum at 2 ug, iv administered as single dose measured after 12 to 24 hrs | 2013 | Journal of medicinal chemistry, Sep-12, Volume: 56, Issue:17 | Synthesis and biological evaluation of α-galactosylceramide analogues with heteroaromatic rings and varying positions of a phenyl group in the sphingosine backbone. |
| AID411368 | Induction of cell proliferation in NOD mouse iNKT cells at 100 ng/mL after 24 hrs by CFSE dilution | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID661322 | Activation of Namalwa cell expressing CD1D-TCR in human MAD11 cells assessed as TH2-mediated IL-13 secretion after 48 hrs by ELISA relative to KRN7000 | 2012 | Journal of medicinal chemistry, Feb-09, Volume: 55, Issue:3 | 3-fluoro- and 3,3-difluoro-3,4-dideoxy-KRN7000 analogues as new potent immunostimulator agents: total synthesis and biological evaluation in human invariant natural killer T cells and mice. |
| AID327253 | Induction of MCP1 secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID277793 | Stimulation of IL4 secretion from C57BL/6 mouse splenocytes at 32 ng/mL after 72 hrs | 2007 | Journal of medicinal chemistry, Feb-08, Volume: 50, Issue:3 | Synthesis and evaluation of 1,2,3-triazole containing analogues of the immunostimulant alpha-GalCer. |
| AID327262 | Induction of IL13 secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID411361 | Activation of iNKT cells in NOD mouse assessed as intracellular cytokine expression at 5 or 10 ug, ip by FACS analysis | 2008 | Bioorganic & medicinal chemistry letters, Dec-15, Volume: 18, Issue:24 | Alpha-S-GalCer: synthesis and evaluation for iNKT cell stimulation. |
| AID421564 | Regulation of immune response in C57BL/6J mouse assessed as induction of NKT cell cytokine response-related IFN-gamma secretion at 10 to 1000 ug/kg, ip after 2 hrs by ELISA | 2009 | Journal of medicinal chemistry, Aug-13, Volume: 52, Issue:15 | Focus on the controversial activation of human iNKT cells by 4-deoxy analogue of KRN7000. |
| AID1650380 | Binding affinity to CD1d in C57BL/6 mouse splenocytes assessed as iNKT cell stimulating activity by measuring induction of Th1-cytokine, IFN-gamma production incubated for 48 hrs by ELISA | 2020 | Bioorganic & medicinal chemistry, 01-01, Volume: 28, Issue:1 | Synthesis and biological activities of amino acids functionalized α-GalCer analogues. |
| AID327259 | Induction of IL4 secretion in human CD161+ CD3+ NKT cells at 10 ug/ml after 18 hrs relative to basal level | 2007 | Proceedings of the National Academy of Sciences of the United States of America, Jun-19, Volume: 104, Issue:25 | Potent immune-modulating and anticancer effects of NKT cell stimulatory glycolipids. |
| AID760651 | Immunostimulatory activity in C57BL/6J mouse assessed as increase in production of IL-4 in serum at 2 ug, iv measured at 3 hrs by cytometric bead array method | 2013 | Bioorganic & medicinal chemistry, Jun-01, Volume: 21, Issue:11 | RCAI-61 and related 6'-modified analogs of KRN7000: their synthesis and bioactivity for mouse lymphocytes to produce interferon-γ in vivo. |
| AID140771 | Lymphocyte Proliferation Stimulatory effect on Allogenic MLR at 1 ng/tritium-thymidine) uptake (percent of control) | 1995 | Journal of medicinal chemistry, Jun-09, Volume: 38, Issue:12 | Structure-activity relationship of alpha-galactosylceramides against B16-bearing mice. |
| [information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||||
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 13 (1.55) | 18.2507 |
| 2000's | 315 (37.46) | 29.6817 |
| 2010's | 443 (52.68) | 24.3611 |
| 2020's | 70 (8.32) | 2.80 |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
According to the monthly volume, diversity, and competition of internet searches for this compound, as well the volume and growth of publications, there is estimated to be moderate demand-to-supply ratio for research on this compound.
| This Compound (27.62) All Compounds (24.57) |
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 23 (2.69%) | 5.53% |
| Reviews | 58 (6.78%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 775 (90.54%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||
| Trial | Phase | Enrollment | Study Type | Start Date | Status | ||
|---|---|---|---|---|---|---|---|
| A Phase 1/2a, Open-Label, Multicenter, Dose-Escalation Study to Evaluate the Safety and Tolerability of Intravenous Administration of RGI-2001 in Patients Undergoing Allogeneic Hematopoietic Stem Cell Transplantation (AHSCT) [NCT01379209] | Phase 1/Phase 2 | 68 participants (Actual) | Interventional | 2011-09-30 | Completed | ||
| Phase I/II Trial of Combination of Lenalidomide (Revlimid, LEN) and Autologous Mature Dendritic Cells Pulsed With α-galactosyl Ceramide (α-GalCer; KRN7000) in Myeloma [NCT00698776] | Phase 1 | 6 participants (Actual) | Interventional | 2009-04-30 | Completed | ||
| Phase I/II Trial of KRN7000 in Patients With Chronic Hepatitis C Infection [NCT00352235] | Phase 1/Phase 2 | 36 participants | Interventional | 2003-08-31 | Completed | ||
| An Open Label Phase 2, Study to Evaluate the Safety and Efficacy of RGI-2001 for the Prevention of Acute Graft-vs-Host Disease Compared to Contemporary Controls in Subjects Following Allogeneic Hematopoietic Stem Cell Transplantation [NCT04014790] | Phase 2 | 49 participants (Actual) | Interventional | 2019-11-25 | Completed | ||
| Phase I/II Trial of KRN7000 in Patients With Chronic Hepatitis B Infection [NCT00363155] | Phase 1/Phase 2 | 28 participants | Interventional | 2003-03-31 | Completed | ||
| Phase I Study of KRN7000 in Patients With Solid Tumor Treated With a Weekly Intravenous Administration Schedule [NCT00003985] | Phase 1 | 0 participants (Actual) | Interventional | 1998-09-30 | Withdrawn | ||
| [information is prepared from clinicaltrials.gov, extracted Sep-2024] | |||||||