117279-73-9
Chemical Structure
Israpafant
Synonym(s): Y 24180
- CAS No.: 117279-73-9
- Formula:C28H29ClN4S
- Molecular Weight:489.07
IUPAC Name: 4-(2-chlorophenyl)-2-(4-isobutylphenethyl)-6,9-dimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine
InChIKey: RMSWMRJVUJSDGN-UHFFFAOYSA-N
SMILES: CC1=NN=C2N1C3=C(C(C4=C(Cl)C=CC=C4)=NC2C)C=C(S3)CCC5=CC=C(C=C5)CC(C)C
Biological Activity: 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].
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Israpafant | 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. | |||||||||||||||||||||
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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. [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.
