SCH 79797 is a non-peptide antagonist of proteinase-activated receptor 1 (PAR1). It blocks binding of the high affinity thrombin receptor-activating peptide (haTRAP) (IC50 = 70 nM) as well as platelet aggregation induced by either haTRAP or α-thrombin (IC50 = 0.3 and 3 μM, respectively). SCH 79797 has no activity against PAR2, PAR4, or other receptors involved in platelet activation. It also blocks PAR1 activation on vascular smooth muscle cells and endothelial cells.
N3-Cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine Dihydrochloride is a selective PAR1 antagonist which was shown to limit myocardial ischemia/reperfusion injury in rat hearts.
SCH 79797 Dihydrochloride is a selective PAR1 antagonist.