117279-73-9

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].

[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.