sch-79797

Description: SCH-79797 is a novel, potent and selective PAR1 (protease activated receptor 1) antagonist with an IC50 of 70 nM and a Ki of 35 nM. SCH-79797 limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 uM. SCH 79797 protects against ischemia/reperfusion-induced arrhythmias in the rat hearts. SCH 79797 and its N-methyl analogue (SCH 203099) inhibited binding of a high-affinity thrombin receptor-activating peptide ((3)HhaTRAP, Ala-Phe(p-F)-Arg-ChA-HArg-(3)HTyr-NH(2)) to PAR-1 with IC(50) values of 70 and 45 nM, respectively.

References: Ahn HS, et al. Inhibition of cellular action of thrombin by N3-cyclopropyl-7-4-(1-methylethyl)phenylmethyl-7H-pyrrolo3, 2-fquinazoline-1, 3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist. Biochem Pharmacol. 2000 Nov 15; 60(10):1425-34; Strande JL, Hsu A, Su J, Fu X, Gross GJ, Baker JE. SCH 79797, a selective PAR1 antagonist, limits myocardial ischemia/reperfusion injury in rat hearts. Basic Res Cardiol. 2007 Jul; 102(4):350-8. Epub 2007 Apr 30. PubMed PMID: 17468933; PubMed Central PMCID: PMC3942648.

Related CAS #: 1216720-69-2 (diHCl salt)