Israpafant
Israpafant Basic information
- Product Name:
- Israpafant
- Synonyms:
-
- Israpafant
- Y 24180
- 4-(2-Chlorophenyl)-2-[2-(4-isobutylphenyl)ethyl]-6,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
- Y-24180;Y24180
- Israpafant (Y-24180
- 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine, 4-(2-chlorophenyl)-6,9-dimethyl-2-[2-[4-(2-methylpropyl)phenyl]ethyl]-
- 7-(2-chlorophenyl)-9,13-dimethyl-4-[2-[4-(2-methylpropyl)phenyl]ethyl]-3-thia-1,8,11,12-tetrazatricyclo[8.3.0.02,6]trideca-2(6),4,7,10,12-pentaene
- Benzaldehyde,5-methoxy-4-nitro-
- CAS:
- 117279-73-9
- MF:
- C28H29ClN4S
- MW:
- 489.07
- Mol File:
- 117279-73-9.mol
Israpafant Chemical Properties
- Melting point:
- 129.5-131.5°
Israpafant Usage And Synthesis
Uses
Israpafant (Y-24180) is a potent, selective and long-acting platelet activation factor (PAF) receptor antagonist with IC50s of 0.84 nM and 3.84 nM against PAF-induced human and rabbit platelet aggregation, respectively. Israpafant stimulates both extracellular Ca2+ influx and intracellular Ca2+ release in prostate cancer cells. Israpafant suppresses the allergic cutaneous reactions including eosinophilia, cytokine production, edema and erythema in mice[1][2].
References
[1] Takehara S, et al. Pharmacological actions of Y-24180, a new specific antagonist of platelet activating factor (PAF): II. Interactions with PAF and benzodiazepine receptors. Prostaglandins. 1990 Dec;40(6):571-83. DOI:10.1016/0090-6980(90)90002-d
[2] Jan C R, Chao Y Y. Novel effect of Y-24180, a presumed specific platelet activation factor receptor antagonist, on Ca2+ levels and growth of human prostate cancer cells. Cellular signalling, 2004, 16(8): 959-965.
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