Page last updated: 2024-12-08

cosalane

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

Description

cosalane: active against a variety of HIV-1 strains & against HIV-2; inhibits the binding of gp120 to CD4 cells & of the postbinding events that lead to fusion of the virus with the cell membrane [Medical Subject Headings (MeSH), National Library of Medicine, extracted Dec-2023]

Cross-References

ID SourceID
PubMed CID455040
CHEMBL ID3545883
MeSH IDM0221119

Synonyms (15)

Synonym
nsc-658586
cosalane
nsc640067
5-[1-(3-carboxy-5-chloro-4-hydroxy-phenyl)-4-[(3s,5s,8r,9s,10s,13r,14s,17r)-17-[(1r)-1,5-dimethylhexyl]-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-3-yl]but-1-enyl]-3-chloro-2-hydroxy-benzoic acid
154212-56-3
benzoic acid, 3,3'-[4-(3.beta.,5.alpha.)-cholestan-3-yl-1-butenylidene]bis[5-chloro-6-hydroxy-
benzoic acid, 3,3'-(4-(3beta,5alpha)-cholestan-3-yl-1-butenylidene)bis(5-chloro-6-hydroxy-
5-[1-(3-carboxy-5-chloro-4-hydroxyphenyl)-4-[(3s,5s,8r,9s,10s,13r,14s,17r)-10,13-dimethyl-17-[(2r)-6-methylheptan-2-yl]-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1h-cyclopenta[a]phenanthren-3-yl]but-1-enyl]-3-chloro-2-hydroxybenzoic acid
2r84y6217j ,
unii-2r84y6217j
benzoic acid, 3,3'-(4-(3.beta.,5.alpha.)-cholestan-3-yl-1-butenylidene)bis(5-chloro-6-hydroxy-
DTXSID00165567
CHEMBL3545883
Q27255501
AKOS040745682

Research Excerpts

Overview

Csalane proved to be a potent inhibitor of HIV with a broad range of activity against a variety of laboratory, drug-resistant, and clinical HIV-1 isolates, HIV-2, and Rauscher murine leukemia virus. Cosalane is a potent inhibitors of HIV replication with multiple sites of action.

ExcerptReferenceRelevance
"Cosalane is a potent inhibitor of HIV replication with activity against a broad range of viral targets. "( Enhanced transport of a novel anti-HIV agent--cosalane and its congeners across human intestinal epithelial (Caco-2) cell monolayers.
Cushman, M; Hejchman, E; Mitra, AK; Pal, D; Patel, J; Udata, C, 2003
)
2.02
"Cosalane proved to be a potent inhibitor of HIV with a broad range of activity against a variety of laboratory, drug-resistant, and clinical HIV-1 isolates, HIV-2, and Rauscher murine leukemia virus."( Design, synthesis, and biological evaluation of cosalane, a novel anti-HIV agent which inhibits multiple features of virus reproduction.
Bader, JP; Buckheit, RW; Clanton, DJ; Cushman, M; Golebiewski, WM; Graham, L; Haugwitz, RD; McMahon, JB; Rice, WG; Weislow, O, 1994
)
1.27
"Cosalane is a potent inhibitor of HIV replication with a broad range of activity. "( Disposition of cosalane, a novel anti-HIV agent, in isolated perfused rat livers.
Badr, MZ; Mitra, AK; Udata, C, 1999
)
2.1
"Cosalane is a potent inhibitor of HIV replication with activity against a broad range of viral targets. "( Transport of cosalane-a highly lipophilic novel anti-HIV agent-across caco-2 cell monolayers.
Mitra, AK; Pal, D; Udata, C, 2000
)
2.12
"Cosalane is a potent inhibitor of HIV replication with multiple sites of action. "( Binding of cosalane--a novel highly lipophilic anti-HIV agent--to albumin and glycoprotein.
Ahmed, MS; Johnston, TP; Kuchimanchi, KR; Mitra, AK, 2001
)
2.14

Bioavailability

The purpose of this study was to investigate the pharmacokinetic disposition of the diglycine (GC) and the diaspartic acid (ASPC) conjugates of cosalane in male Sprague-Dawley rats. It was concluded that the poor oral bioavailability of cosAlane may be due to its poor enterocytic transport coupled with sequestration in liver parenchymal cell membrane layers.

ExcerptReferenceRelevance
" Therefore it was concluded that the poor oral bioavailability of cosalane may be due to its poor enterocytic transport coupled with sequestration in liver parenchymal cell membrane layers."( Pharmacokinetics, biliary excretion, and tissue distribution of novel anti-HIV agents, cosalane and dihydrocosalane, in Sprague-Dawley rats.
Johnston, TP; Kuchimanchi, KR; Mitra, AK; Udata, C, 2000
)
0.77
" However, the oral bioavailability of this highly lipophilic compound is extremely poor (<1%)."( Transport of cosalane-a highly lipophilic novel anti-HIV agent-across caco-2 cell monolayers.
Mitra, AK; Pal, D; Udata, C, 2000
)
0.68
" The purpose of this study was to investigate: (1) the pharmacokinetic disposition of the diglycine (GC) and the diaspartic acid (ASPC) conjugates of cosalane in male Sprague-Dawley rats; (2) intestinal absorption of cosalane and its amino acid conjugates using in vitro (small intestinal segments), in situ (closed loop); and (3) biodistribution of GC and its absolute oral bioavailability in rat."( Intestinal absorption and biodistribution of cosalane and its amino acid conjugates: novel anti-HIV agents.
Cushman, M; Gandhi, MD; Johnston, TP; Kuchimanchi, KR; Mitra, AK; Santhosh, KC; Sheta, RR, 2002
)
0.77
" However, oral bioavailability of this highly lipophilic compound is extremely poor (<1%)."( Enhanced transport of a novel anti-HIV agent--cosalane and its congeners across human intestinal epithelial (Caco-2) cell monolayers.
Cushman, M; Hejchman, E; Mitra, AK; Pal, D; Patel, J; Udata, C, 2003
)
0.58
[information is derived through text-mining from research data collected from National Library of Medicine (NLM), extracted Dec-2023]

Research

Studies (25)

TimeframeStudies, This Drug (%)All Drugs %
pre-19900 (0.00)18.7374
1990's11 (44.00)18.2507
2000's11 (44.00)29.6817
2010's3 (12.00)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: 22.57

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 Index22.57 (24.57)
Research Supply Index3.26 (2.92)
Research Growth Index4.18 (4.65)
Search Engine Demand Index23.28 (26.88)
Search Engine Supply Index2.00 (0.95)

This Compound (22.57)

All Compounds (24.57)

Study Types

Publication TypeThis drug (%)All Drugs (%)
Trials0 (0.00%)5.53%
Reviews1 (4.00%)6.00%
Case Studies0 (0.00%)4.05%
Observational0 (0.00%)0.25%
Other24 (96.00%)84.16%
[information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023]