cosalane
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 Source | ID |
|---|---|
| PubMed CID | 455040 |
| CHEMBL ID | 3545883 |
| MeSH ID | M0221119 |
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.
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.
| Excerpt | Reference | Relevance |
|---|---|---|
| " 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 |
Research
Studies (25)
| Timeframe | Studies, This Drug (%) | All Drugs % |
|---|---|---|
| pre-1990 | 0 (0.00) | 18.7374 |
| 1990's | 11 (44.00) | 18.2507 |
| 2000's | 11 (44.00) | 29.6817 |
| 2010's | 3 (12.00) | 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] | ||
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.
| This Compound (22.57) All Compounds (24.57) |
Study Types
| Publication Type | This drug (%) | All Drugs (%) |
|---|---|---|
| Trials | 0 (0.00%) | 5.53% |
| Reviews | 1 (4.00%) | 6.00% |
| Case Studies | 0 (0.00%) | 4.05% |
| Observational | 0 (0.00%) | 0.25% |
| Other | 24 (96.00%) | 84.16% |
| [information is prepared from research data collected from National Library of Medicine (NLM), extracted Dec-2023] | ||