7H-Pyrrolo[3,2-f]quinazoline-1,3-diaMine, N3-cyclopropyl-7-[[4-(1-Methylethyl)phenyl]Methyl]-, (Hydrochloride) (1:2)

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.

SCH 79797 Dihydrochloride is a selective PAR1 antagonist.

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.

PAR1

Desiccate at RT

[1] HO-SAM AHN. Structure-activity relationships of pyrroloquinazolines as thrombin receptor antagonists[J]. Bioorganic & Medicinal Chemistry Letters, 1999, 9 14: Pages 2073-2078. DOI: 10.1016/s0960-894x(99)00339-x
[2] HO-SAM AHN . Inhibition of cellular action of thrombin by N3-cyclopropyl-7-{[4-(1-methylethyl)phenyl]methyl}-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine (SCH 79797), a nonpeptide thrombin receptor antagonist[J]. Biochemical pharmacology, 2000, 60 10: Pages 1425-1434. DOI: 10.1016/s0006-2952(00)00460-3
[3] ELAINE A LIDINGTON. A role for proteinase-activated receptor 2 and PKC-epsilon in thrombin-mediated induction of decay-accelerating factor on human endothelial cells.[J]. American journal of physiology. Cell physiology, 2005, 289 6: C1437-47. DOI: 10.1152/ajpcell.00502.2004