245520-69-8
Chemical Structure
SCH79797
- CAS No.: 245520-69-8
- Formula:C23H25N5
- Molecular Weight:371.48
IUPAC Name: N3-cyclopropyl-7-(4-isopropylbenzyl)-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine
InChIKey: AVXQPEKZIGPIJW-UHFFFAOYSA-N
SMILES: NC1=NC(NC2CC2)=NC3=CC=C(N(CC4=CC=C(C(C)C)C=C4)C=C5)C5=C31
Biological Activity: SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes[1][2][3][4].
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SCH79797 | 99.74% | SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes. | ||||||||||||||||||||
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SCH79797 (Standard) | ≥98% | SCH79797 (Standard) is the analytical standard of SCH79797. This product is intended for research and analytical applications. SCH79797 is a highly potent, selective nonpeptide protease activated receptor 1 (PAR1) antagonist. SCH79797 inhibits binding of a high-affinity thrombin receptor-activating peptide to PAR1 with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. SCH79797 has antiproliferative and pro-apoptotic effects, and limits myocardial ischemia/reperfusion injury in rat hearts. SCH79797 also potently prevents PAR1 activation in vascular smooth muscle cells, endothelial cells, and astrocytes. | ||||||||||||||||||||
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- [1]. Ahn HS, et al. 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. Biochem Pharmacol. 2000 Nov 15;60(10):1425-34. [Content Brief]
- [2]. Di Serio C, et al. Protease-activated receptor 1-selective antagonist SCH79797 inhibits cell proliferation and induces apoptosis by a protease-activated receptor 1-independent mechanism. Basic Clin Pharmacol Toxicol. 2007 Jul;101(1):63-9. [Content Brief]
- [3]. Sokolova E, et al. A novel therapeutic target in various lung diseases: airway proteases and protease-activated receptors. Pharmacol Ther. 2007 Jul;115(1):70-83. [Content Brief]
- [4]. Strande JL, et al. SCH 79797, a selective PAR1 antagonist, limits myocardial ischemia/reperfusion injury in rat hearts. Basic Res Cardiol. 2007 Jul;102(4):350-8. [Content Brief]
Keywords
