Page last updated: 2024-10-15

loxoribine

Cross-References

ID SourceID
PubMed CID135410906
CHEMBL ID292008
SCHEMBL ID61782
SCHEMBL ID16516342
MeSH IDM0187463

Synonyms (54)

Synonym
loxoribine
rwj-21757
7a8ogua
loxoribine (usan/inn)
121288-39-9
D04787
7-allyl-7,8-dihydro-8-oxoguanosine, 95%
rwj 21757
7-allyl-8-oxoguanosine
CHEMBL292008
2-amino-9-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-7-prop-2-enyl-3h-purine-6,8-dione
dtxsid3046748 ,
cas-121288-39-9
tox21_112592
dtxcid1026748
loxoribine [usan:inn]
7-allyl-2-amino-9-beta-d-ribofuranosylpurine-6,8(1h,9h)-dione
loxoribina [inn-spanish]
loxoribinum [inn-latin]
loxoribina
unii-9cas0v66oi
guanosine, 7,8-dihydro-8-oxo-7-(2-propenyl)-
loxoribinum
9cas0v66oi ,
7-allyl-7,8-dihydro-8-oxoguanosine
2-amino-9-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-7-(prop-2-en-1-yl)-6,7,8,9-tetrahydro-3h-purine-6,8-dione
gtpl5018
7-allyl-7,8-dihydro-8-oxo-guanosine
loxoribine [usan]
loxoribine [inn]
SCHEMBL61782
NCGC00263547-01
tox21_112592_1
SCHEMBL16516342
VDCRFBBZFHHYGT-IOSLPCCCSA-N
7-allyl-2-amino-9-((2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)-tetrahydrofuran-2-yl)-1h-purine-6,8(7h,9h)-dione
AKOS024284397
7,8-dihydro-8-oxo-7-(2-propenyl)guanosine
sr-01000883708
SR-01000883708-1
(loxoribine)
7-allyl-2-amino-9-((2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)tetrahydrofuran-2-yl)-1h-purine-6,8(7h,9h)-dione
SDL ,
2-azanyl-9-[(2~{r},3~{r},4~{s},5~{r})-5-(hydroxymethyl)-3,4-bis(oxidanyl)oxolan-2-yl]-7-prop-2-enyl-1~{h}-purine-6,8-dione
7-allyl-78-dihydro-8-oxoguanosine
HMS3677D12
CS-0028896
HY-108472
Q27081526
HMS3413D12
rwj 217577-allyl-8-oxoguanosine
2-amino-9-[(2r,3r,4s,5r)-3,4-dihydroxy-5-(hydroxymethyl)oxolan-2-yl]-7-prop-2-enyl-1h-purine-6,8-dione
7,8-dihydro-8-oxo-7-allyl-guanosine
AKOS040741970

Research Excerpts

Overview

Loxoribine is a potent new immunostimulant with a relatively broad spectrum of immunobiological activities.

ExcerptReference
"Loxoribine is a potent new immunostimulant with a relatively broad spectrum of immunobiological activities. "( A new approach to vaccine adjuvants. Immunopotentiation by intracellular T-helper-like signals transmitted by loxoribine.
Goodman, MG, 1995
)

Treatment

Loxoribine treatment enhanced both the NK and LAK activity of cells from individuals with low and high spontaneous NK activity. Group showed marked regression of both epithelial and stromal components.

ExcerptReference
"Loxoribine treatment enhanced both the NK and LAK activity of cells from individuals with low and high spontaneous NK activity."( Murine strain variation in the natural killer cell and proliferative responses to the immunostimulatory compound 7-allyl-8-oxoguanosine: role of cytokines.
Chourmouzis, E; Goodman, MG; Lee, S; MacIntyre, JP; Pope, BL, 1994
)
"The loxoribine-treated group showed marked regression of both epithelial and stromal components. "( Regression of endometrial explants in a rat model of endometriosis treated with the immune modulators loxoribine and levamisole.
Bukovsky, A; Caudle, MR; Chen, TT; Keenan, JA; Massey, PJ; Williams-Boyce, PK, 1999
)

Bioavailability

ExcerptReference
"The ATP-binding cassette transporter P-glycoprotein (P-gp) is known to limit both brain penetration and oral bioavailability of many chemotherapy drugs."( A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
Ambudkar, SV; Brimacombe, KR; Chen, L; Gottesman, MM; Guha, R; Hall, MD; Klumpp-Thomas, C; Lee, OW; Lee, TD; Lusvarghi, S; Robey, RW; Shen, M; Tebase, BG, 2019
)

Dosage Studied

ExcerptReference
" In murine B cells, two distinct binding activities have been characterized that have dissociation constants that parallel their distinctive dose-response profiles."( Topology of the loxoribine binding site. Studies with inactive loxoribine analogues.
Goodman, JH; Goodman, MG, 1994
)
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Protein Targets (1)

Potency Measurements

ProteinTaxonomyMeasurementAverage (µ)Min (ref.)Avg (ref.)Max (ref.)Bioassay(s)
RAR-related orphan receptor gammaMus musculus (house mouse)Potency28.60080.006038.004119,952.5996AID1159521; AID1159523
[prepared from compound, protein, and bioassay information from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (56)

Assay IDTitleYearJournalArticle
AID1346987P-glycoprotein substrates identified in KB-8-5-11 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347154Primary screen GU AMC qHTS for Zika virus inhibitors2020Proceedings of the National Academy of Sciences of the United States of America, 12-08, Volume: 117, Issue:49
Therapeutic candidates for the Zika virus identified by a high-throughput screen for Zika protease inhibitors.
AID1296008Cytotoxic Profiling of Annotated Libraries Using Quantitative High-Throughput Screening2020SLAS discovery : advancing life sciences R & D, 01, Volume: 25, Issue:1
Cytotoxic Profiling of Annotated and Diverse Chemical Libraries Using Quantitative High-Throughput Screening.
AID1508630Primary qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1346986P-glycoprotein substrates identified in KB-3-1 adenocarcinoma cell line, qHTS therapeutic library screen2019Molecular pharmacology, 11, Volume: 96, Issue:5
A High-Throughput Screen of a Library of Therapeutics Identifies Cytotoxic Substrates of P-glycoprotein.
AID1347097qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347100qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for LAN-5 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508627Counterscreen qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: GLuc-NoTag assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347094qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347107qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh30 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347090qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347101qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347086qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lymphocytic Choriomeningitis Arenaviruses (LCMV): LCMV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID651635Viability Counterscreen for Primary qHTS for Inhibitors of ATXN expression
AID1347425Rhodamine-PBP qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347096qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for U-2 OS cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347089qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1745845Primary qHTS for Inhibitors of ATXN expression
AID1347407qHTS to identify inhibitors of the type 1 interferon - major histocompatibility complex class I in skeletal muscle: primary screen against the NCATS Pharmaceutical Collection2020ACS chemical biology, 07-17, Volume: 15, Issue:7
High-Throughput Screening to Identify Inhibitors of the Type I Interferon-Major Histocompatibility Complex Class I Pathway in Skeletal Muscle.
AID1347106qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for control Hh wild type fibroblast cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347082qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: LASV Primary Screen - GLuc reporter signal2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347098qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-SH cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508629Cell Viability qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347103qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347102qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh18 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347099qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347091qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347108qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Rh41 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1508628Confirmatory qHTS for small molecule stabilizers of the endoplasmic reticulum resident proteome: Secreted ER Calcium Modulated Protein (SERCaMP) assay2021Cell reports, 04-27, Volume: 35, Issue:4
A target-agnostic screen identifies approved drugs to stabilize the endoplasmic reticulum-resident proteome.
AID1347105qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for MG 63 (6-TG R) cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347093qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347083qHTS for Inhibitors of the Functional Ribonucleoprotein Complex (vRNP) of Lassa (LASV) Arenavirus: Viability assay - alamar blue signal for LASV Primary Screen2020Antiviral research, 01, Volume: 173A cell-based, infectious-free, platform to identify inhibitors of lassa virus ribonucleoprotein (vRNP) activity.
AID1347424RapidFire Mass Spectrometry qHTS Assay for Modulators of WT P53-Induced Phosphatase 1 (WIP1)2019The Journal of biological chemistry, 11-15, Volume: 294, Issue:46
Physiologically relevant orthogonal assays for the discovery of small-molecule modulators of WIP1 phosphatase in high-throughput screens.
AID1347104qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347095qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID1347092qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells2018Oncotarget, Jan-12, Volume: 9, Issue:4
Quantitative high-throughput phenotypic screening of pediatric cancer cell lines identifies multiple opportunities for drug repurposing.
AID119667In vivo natural killer cell response in splenocytes of mice injected with 2 mg intravenous dose. % lysis of YAC-1 cells at effector: target ratio of 50:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID140774Augment antibody response of B cells to sheep red blood cell (SRBC) challenge (adjuvanticity)1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID220083Stimulation of natural killer (NK) response in Yac-1 cell line (mouse, lymphoma)1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID119550In vivo natural killer cell response in splenocytes of mice injected with 2 mg intravenous dose. % lysis of YAC-1 cells at effector: target ratio of 200:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID119672In vivo natural killer cell response in splenocytes of mice injected with 2 mg parenteral dose. % lysis of YAC-1 cells at effector: target ratio of 25:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID119673In vivo natural killer cell response in splenocytes of mice injected with 2 mg parenteral dose. % lysis of YAC-1 cells at effector: target ratio of 50:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID144275In vitro Natural Killer cell activity (Activation of murine splenocyte NK cells by its ability to lyze YAC-1 target cells in chromium release assay) relative to interleukin 2 at 10E-4 to 10E-12 M conc.1998Journal of medicinal chemistry, May-21, Volume: 41, Issue:11
Synthesis and activity of dipeptides, linked to targeting ligands, as specific NK cell enhancers.
AID220086Percent of maximum response was tested for its ability to stimulate the natural killer response in murine in vitro cell assays1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID119676In vivo natural killer cell response in splenocytes of mice injected with 2 mg subcutaneous dose. % lysis of YAC-1 cells at effector: target ratio of 25:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID119669In vivo natural killer cell response in splenocytes of mice injected with 2 mg parenteral dose % lysis of YAC-1 cells at effector: target ratio of 200:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID119547In vivo natural killer cell response in splenocytes of mice injected with 2 mg intravenous dose % lysis of YAC-1 cells at effector: target ratio of 25:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID119675In vivo natural killer cell response in splenocytes of mice injected with 2 mg subcutaneous dose. % lysis of YAC-1 cells at effector: target ratio of 200:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID140780Percent of maximum response was tested to augment the antibody response of B cells to sheep red blood cell challenge1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID119674In vivo natural killer cell response in splenocytes of mice injected with 2 mg subcutaneous dose. % lysis of YAC-1 cells at effector: target ratio of 100:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID119671In vivo natural killer cell response in splenocytes of mice injected with 2 mg parenteral dose. % lysis of YAC-1 cells at effector: target ratio of 100:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID142466Ability to act as B-cell mitogens1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID119677In vivo natural killer cell response in splenocytes of mice injected with 2 mg subcutaneous dose. % lysis of YAC-1 cells at effector: target ratio of 50:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID142474Percent of maximum response was tested for its ability to act as B-cell mitogens (mitogenicity)1994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID119549In vivo natural killer cell response in splenocytes of mice injected with 2 mg intravenous dose. % lysis of YAC-1 cells at effector: target ratio of 100:11994Journal of medicinal chemistry, Oct-14, Volume: 37, Issue:21
Small-molecule immunostimulants. Synthesis and activity of 7,8-disubstituted guanosines and structurally related compounds.
AID1345471Human TLR7 (Toll-like receptor family)2003European journal of immunology, Nov, Volume: 33, Issue:11
The Toll-like receptor 7 (TLR7)-specific stimulus loxoribine uncovers a strong relationship within the TLR7, 8 and 9 subfamily.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (74)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's18 (24.32)18.2507
2000's27 (36.49)29.6817
2010's21 (28.38)24.3611
2020's8 (10.81)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials1 (1.35%)5.53%
Reviews3 (4.05%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other70 (94.59%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]