Page last updated: 2024-12-11

cyclosporin h

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

Description

cyclosporin H: non-immunophilin-binding cyclosporin; RN given for (D)-Val [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID6476564
CHEMBL ID4448165
MeSH IDM0143093

Synonyms (24)

Synonym
cyclosporin a, 5-(n-methyl-d-valine)-
cyclosporin h
12-((4e)(1r,2r)-1-hydroxy-2-methylhex-4-enyl)(6s,12s,15s,21s,24s,27s,30s,3r,9r,33r)-9,24-bis(methylethyl)-15-ethyl-2,5,8,11,17,20,26,30,33-nonamethyl-3,6,21,27-tetrakis(2-methylpropyl)-2,5,8,11,14,17,20,23,26,29,32-undecaazacyclotritriacontane-1,4,7,10,13
(3r,6s,9s,12r,15s,18s,21s,24s,30s,33s)-30-ethyl-33-[(e,1r,2r)-1-hydroxy-2-methyl-hex-4-enyl]-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecazacyclotritriacontane-2,5,8,11,14,17,20,23,26,29,3
[d-meval]11-csa
5-(n-methyl-d-valine)cyclosporine a
cyclosporine h
csh cyclosporin
unii-fuo6o3ndnh
fuo6o3ndnh ,
5-(n-methyl-d-valine)cyclosporin a
cyclosporin h, (-)-
sandoz-37-839
mfcd04039488
CHEMBL4448165
NCGC00386167-01
(3r,6s,9s,12r,15s,18s,21s,24s,30s,33s)-30-ethyl-33-((1r,2r,e)-1-hydroxy-2-methylhex-4-en-1-yl)-6,9,18,24-tetraisobutyl-3,21-diisopropyl-1,4,7,10,12,15,19,25,28-nonamethyl-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2,5,8,11,14,17,20,23,26,29
EX-A2225
PMATZTZNYRCHOR-JLPRAAIDSA-N
DTXSID801017527
CS-0027967
Q27278214
D83129
HY-P1122

Research Excerpts

Effects

ExcerptReferenceRelevance
"As cyclosporin H has no immunosuppressive activity, these data indicate that the inhibitory effect of the cyclosporin derivatives on NO synthase expression is not related to the immunosuppressive action of the drugs."( Cyclosporin derivatives inhibit interleukin 1 beta induction of nitric oxide synthase in renal mesangial cells.
Kunz, D; Mühl, H; Pfeilschifter, J; Rob, P, 1993
)
0.8

Bioavailability

ExcerptReferenceRelevance
"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
)
0.51

Dosage Studied

ExcerptRelevanceReference
" CsH was observed to reduce both the number and DNA synthesis of EK in a statistically significant manner at the dosage of 5 micrograms/ml after 24, 48 and 72 h in culture."( Nonimmunosuppressive ciclosporin H inhibits the growth and DNA synthesis of cultured normal human epidermal keratinocytes.
Castells-Rodellas, A; Faure, M; Haftek, M; Kanitakis, J; Ramirez-Bosca, A; Thivolet, J, 1989
)
0.28
" In vitro, the dose-response curves to MP were examined in pretransplant PHA cultures."( The impact of high lymphocyte sensitivity to glucocorticoids on kidney graft survival in patients treated with azathioprine and cyclosporine.
Ladefoged, J; Langhoff, E, 1987
)
0.27
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Bioassays (8)

Assay IDTitleYearJournalArticle
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.
AID1347159Primary screen GU Rhodamine qHTS for Zika virus inhibitors: Unlinked NS2B-NS3 protease assay2020Proceedings 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.
AID1347160Primary screen NINDS Rhodamine 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.
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.
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.
AID1532161Thermodynamic aqueous solubility of compound in pH 7.4 PBS by UPLC-MS analysis2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Lipophilic Permeability Efficiency Reconciles the Opposing Roles of Lipophilicity in Membrane Permeability and Aqueous Solubility.
AID1532163Apparent permeability in low-efflux MDCK2 cells at 2 uM by lucifer yellow dye-based UPLC-MS analysis2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Lipophilic Permeability Efficiency Reconciles the Opposing Roles of Lipophilicity in Membrane Permeability and Aqueous Solubility.
AID15321621,9-decadiene/aqueous buffer solution partition coefficient, log D of the compound in PBS at pH 7.4 by shake flask method2018Journal of medicinal chemistry, 12-27, Volume: 61, Issue:24
Lipophilic Permeability Efficiency Reconciles the Opposing Roles of Lipophilicity in Membrane Permeability and Aqueous Solubility.
[information is prepared from bioassay data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (62)

TimeframeStudies, This Drug (%)All Drugs %
pre-19908 (12.90)18.7374
1990's18 (29.03)18.2507
2000's14 (22.58)29.6817
2010's18 (29.03)24.3611
2020's4 (6.45)2.80
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Market Indicators

Research Demand Index: 30.12

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.

MetricThis Compound (vs All)
Research Demand Index30.12 (24.57)
Research Supply Index4.14 (2.92)
Research Growth Index4.78 (4.65)
Search Engine Demand Index30.68 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (30.12)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews0 (0.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other62 (100.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]