Israpafant  (Synonyms: Y 24180)

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].

IC50: 0.84 nM (PAF-induced human platelet aggregation), 3.84 nM (PAF-induced rabbit platelet aggregation)^[1]

489.07

C₂₈H₂₉ClN₄S

117279-73-9

CC1=NN=C2N1C3=C(C(C4=C(Cl)C=CC=C4)=NC2C)C=C(S3)CCC5=CC=C(C=C5)CC(C)C

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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.  [Content Brief]

  [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.