Page last updated: 2024-12-10

kh 1060

Description Research Excerpts Clinical Trials Roles Classes Pathways Study Profile Bioassays Related Drugs Related Conditions Protein Interactions Research Growth Market Indicators

Description

KH 1060: structure given in first source; a new 20-epi-vitamin D3 analog [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID5288670
CHEMBL ID432600
SCHEMBL ID2917
MeSH IDM0200606

Synonyms (36)

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

Research Excerpts

Overview

KH 1060 is a 20-epi analogue of 1,25-dihydroxyvitamin D3. It is a potent agonist of the vitamin D receptor.

ExcerptReferenceRelevance
"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

Compound-Compound Interactions

ExcerptReferenceRelevance
"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

Dosage Studied

ExcerptRelevanceReference
" 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
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (5)

Assay IDTitleYearJournalArticle
AID103218In vitro activity on human breast adenocarcinoma cell line MCF-7 proliferation2000Journal 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.
AID260130Inhibition of transactivation of human VDR in COS7 cells2006Journal of medicinal chemistry, Feb-23, Volume: 49, Issue:4
Vitamin D receptor: ligand recognition and allosteric network.
AID213723Relative differentiating activity of U 937 cells when the reference value of 1,25-(OH)3D3 is defined as 1.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Conformation-function relationship of vitamin D: conformational analysis predicts potential side-chain structure.
AID213718Relative differentiating activity of U 937 cells when the reference value of 1,25-(OH)3D3 is defined as 1.1998Journal of medicinal chemistry, Apr-23, Volume: 41, Issue:9
Conformation-function relationship of vitamin D: conformational analysis predicts potential side-chain structure.
AID260131Antagonistic activity against human VDR in presence of 1,25(OH)2D32006Journal 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]

Research

Studies (79)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's58 (73.42)18.2507
2000's19 (24.05)29.6817
2010's2 (2.53)24.3611
2020's0 (0.00)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 14.82

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.

MetricThis Compound (vs All)
Research Demand Index14.82 (24.57)
Research Supply Index4.44 (2.92)
Research Growth Index4.08 (4.65)
Search Engine Demand Index10.37 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (14.82)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials4 (5.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other76 (95.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]