KH 1060: structure given in first source; a new 20-epi-vitamin D3 analog
ID Source | ID |
---|---|
PubMed CID | 5288670 |
CHEMBL ID | 432600 |
SCHEMBL ID | 2917 |
MeSH ID | M0200606 |
Synonym |
---|
LMST03020432 |
1alpha,25-dihydroxy-26,27-dimethyl-24a-homo-22-oxa-20-epivitamin d3 / 1alpha,25-dihydroxy-26,27-dimethyl-24a-homo-22-oxa-20-epicholecalciferol |
(5z,7e)-(1s,3r,20r)-26,27-dimethyl-24a-homo-22-oxa-9,10-seco-5,7,10(19)-cholestatriene-1,3,25-triol |
HY-32340 |
gtpl2775 |
1alpha,25-(oh),-20-epi-22-oxa-24,26,27-trishomovitamin d |
lexacalcitol |
kh-1060 |
KH1 , |
5-(2-{1-[1-(4-ethyl-4-hydroxy-hexyloxy)-ethyl]-7a-methyl-octahydro-inden-4-ylidene}-ethylidene)-4-methylene-cyclohexane-1,3-diol |
DB03451 |
kh 1060 |
(5z,7e,20r)-20-((4-ethyl-4-hydroxyhexyl)oxy)-9,10-secopregna-5,7,10(19)-triene-1alpha,3beta-diol |
1,3-cyclohexanediol, 5-((1-(1-((4-ethyl-4-hydroxyhexyl)oxy)ethyl)octahydro-7a-methyl-4h-inden-4-ylidene)ethylidene)-4-methylene-, (1s-(1alpha(s*),3abeta,4e(1s*,3r*,5z),7aalpha))- |
kh1060 |
20-epi-22-oxa-24a-homo-26,27-dimethyl-1alpha,25-dihydroxyvitamin d3 |
lexacalcitol [inn] |
131875-08-6 |
CHEMBL432600 |
(1r,3s,5z)-5-[(2e)-2-[(1s,3as,7as)-1-[(1r)-1-(4-ethyl-4-hydroxyhexoxy)ethyl]-7a-methyl-2,3,3a,5,6,7-hexahydro-1h-inden-4-ylidene]ethylidene]-4-methylidenecyclohexane-1,3-diol |
unii-9g3dca3958 |
9g3dca3958 , |
CS-0399 |
KLZOTDOJMRMLDX-YBBVPDDNSA-N |
SCHEMBL2917 |
(5z,7e,20r)-20-((4-ethyl-4-hydroxyhexyl)oxy)-9,10-secopregna-5,7,10(19)-triene-1.alpha.,3.beta.-diol |
AKOS025312290 |
AC-8889 |
(1s,3r,5z,7e,14beta,17alpha,20r)-20-[(4-ethyl-4-hydroxyhexyl)oxy]-9,10-secopregna-5,7,10-triene-1,3-diol |
'1alpha,25-dihydroxyl-20-epi-22-oxa-24,26,27-trihomo vitamin d3' |
Q27080264 |
4-(methoxycarbonyl)phenylboronicacid |
lexacalcideferol |
F83980 |
MS-28460 |
DTXSID10869807 |
KH 1060 is a 20-epi analogue of 1,25-dihydroxyvitamin D3. It is a potent agonist of the vitamin D receptor.
Excerpt | Reference | Relevance |
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"KH 1060 is a 20-epi-vitamin D3 analogue, structurally related to 1,25-dihydroxyvitamin D3 (1,25(OH)2D3). " | ( Efficacy and safety of the 20-epi-vitamin D3 analogue KH 1060 in the topical therapy of psoriasis: results of a dose-ranging study. Axelsen, MB; Baadsgaard, O; Dam, TN; Grønhøj Larsen, F; Hansen, ER; Kragballe, K; Søndergaard, J, 1994) | 1.98 |
"KH 1060 is a 20-epi analogue of 1,25-dihydroxyvitamin D3 and a potent agonist of the vitamin D receptor. " | ( Enhancement of the granulation tissue formation in hairless mice by a potent vitamin D receptor agonist--KH 1060. Gniadecki, R; Serup, J, 1994) | 1.95 |
Excerpt | Reference | Relevance |
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"We examined the ability of four novel 20-epi-vitamin D3 analogs (CB1093, KH1060, KH1266, and CB1267), either alone or in combination with 9-cis retinoic acid (RA) to inhibit colony growth of a human prostate cancer cell line, LNCaP, using soft agar as well as bone marrow stroma." | ( Novel 20-epi-vitamin D3 analog combined with 9-cis-retinoic acid markedly inhibits colony growth of prostate cancer cells. Binderup, L; Campbell, MJ; Elstner, E; Heber, D; Koeffler, HP; Munker, R; Said, J; Shintaku, P, 1999) | 0.3 |
Excerpt | Relevance | Reference |
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" Dose-response studies showed that KH 1060 was the most potent analogue, because it was able to induce differentiation in all seven breast cancer cell lines (measured by lipid staining) and to suppress more than 50% clonal proliferation (ED50) at 10(-10) M in all cell lines, except MDA-MB-436 and BT-20." | ( 20-epi-vitamin D3 analogues: a novel class of potent inhibitors of proliferation and inducers of differentiation of human breast cancer cell lines. Binderup, L; de Vos, S; Elstner, E; Heber, D; Koeffler, HP; Linker-Israeli, M; Said, J; Shintaku, IP; Umiel, T; Uskokovic, M, 1995) | 0.57 |
" A dose-response analysis showed that a 10(-6) M concentration of this vitamin consistently induced a maximal accumulation of 7-fold over the control cells." | ( Growth inhibition of human breast cancer cells by 1,25-dihydroxyvitamin D3 is accompanied by induction of apolipoprotein D expression. Alvarez, S; Binderup, L; López-Boado, YS; López-Otín, C; Puente, XS; Tolivia, J, 1997) | 0.3 |
" Hormone dose-response relationships for translocation and for transactivation were similar." | ( Hormone-dependent translocation of vitamin D receptors is linked to transactivation. Barsony, J; Racz, A, 1999) | 0.3 |
Assay ID | Title | Year | Journal | Article |
---|---|---|---|---|
AID103218 | In vitro activity on human breast adenocarcinoma cell line MCF-7 proliferation | 2000 | Journal of medicinal chemistry, Sep-21, Volume: 43, Issue:19 | Conceptually new 20-epi-22-oxa sulfone analogues of the hormone 1alpha,25-dihydroxyvitamin D(3): synthesis and biological evaluation. |
AID260130 | Inhibition of transactivation of human VDR in COS7 cells | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | Vitamin D receptor: ligand recognition and allosteric network. |
AID213723 | Relative differentiating activity of U 937 cells when the reference value of 1,25-(OH)3D3 is defined as 1. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9 | Conformation-function relationship of vitamin D: conformational analysis predicts potential side-chain structure. |
AID213718 | Relative differentiating activity of U 937 cells when the reference value of 1,25-(OH)3D3 is defined as 1. | 1998 | Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9 | Conformation-function relationship of vitamin D: conformational analysis predicts potential side-chain structure. |
AID260131 | Antagonistic activity against human VDR in presence of 1,25(OH)2D3 | 2006 | Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4 | Vitamin D receptor: ligand recognition and allosteric network. |
[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 | 58 (73.42) | 18.2507 |
2000's | 19 (24.05) | 29.6817 |
2010's | 2 (2.53) | 24.3611 |
2020's | 0 (0.00) | 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 weak demand-to-supply ratio for research on this compound.
| This Compound (14.82) All Compounds (24.57) |
Publication Type | This drug (%) | All Drugs (%) |
---|---|---|
Trials | 4 (5.00%) | 5.53% |
Reviews | 0 (0.00%) | 6.00% |
Case Studies | 0 (0.00%) | 4.05% |
Observational | 0 (0.00%) | 0.25% |
Other | 76 (95.00%) | 84.16% |
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] |