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SCH79797 dihydrochloride

Catalog No. T12870 CAS 1216720-69-2

SCH79797 dihydrochloride is an effective and selective antagonist of protease activated receptor 1 (PAR1) with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects.

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SCH79797 dihydrochloride, CAS 1216720-69-2

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Purity: 98%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	SCH79797 dihydrochloride is an effective and selective antagonist of protease activated receptor 1 (PAR1) with an IC50 of 70 nM and a Ki of 35 nM. SCH79797 dihydrochloride has antiproliferative and pro-apoptotic effects.
In vitro	SCH79797 dihydrochloride inhibits thrombin-induced platelet aggregation with an IC50 of 3 μM. In NIH 3T3 cells, SCH79797 dihydrochloride inhibits serum-stimulated activation of p44/p42 mitogen-activated protein kinases (MAPK) at low concentrations and induces apoptosis at higher concentrations[1]. SCH79797 dihydrochloride inhibits high-affinity thrombin receptor-activating peptide ([3H]haTRAP) binding in a competitive manner. SCH79797 dihydrochloride inhibits α-thrombin- and haTRAP-induced aggregation of human platelets. Thrombin produces transient increases in cytosolic free Ca2+ concentration ([Ca2+]i) in hCASMC. SCH79797 dihydrochloride effectively inhibits this increase in [Ca2+]i. SCH79797 dihydrochloride completely inhibits Thrombin- and TK-stimulated [3H]thymidine incorporation [4].
In vivo	In male Sprague Dawley rats, SCH79797 dihydrochloride (2.5 μg/kg, 10 μg/kg, 25 μg/kg, 50 μg/kg, 100 μg/kg, and 250 μg/kg; i.v.) reduces myocardial necrosis following I/R in the intact rat heart in two rat models of myocardial ischemia/reperfusion (I/R) injury immediately before or during ischemia[3].

Molecular Weight	444.4
Formula	C23H27Cl2N5
CAS No.	1216720-69-2

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

Ethanol: 10 mg/mL (22.50 mM), Need ultrasonic and warming

DMSO: 20 mg/mL (45.00 mM), Need ultrasonic and warming

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. 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. 2. 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. 3. 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. 4. 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.

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SLIGRL-NH2 TRAP-6 PAR-4 Agonist Peptide, amide acetate PAR-4 Agonist Peptide, amide TFLLR-NH2 Thrombin Receptor Activator for Peptide 5 (TRAP-5) Protease-Activated Receptor-4 AC-264613

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Keywords

SCH79797 dihydrochloride 1216720-69-2 G蛋白偶联受体凋亡其他 Protease-activated Receptor Apoptosis Others infarct SCH-79797 dihydrochloride SCH-79797 SCH79797 Inhibitor inhibit Nonpeptide thrombin wortmannin SCH 79797 antiproliferative platelets Protease Activated Receptor (PAR) pro-apoptotic thrombosis Thrombin receptors PAR1 cardioprotection inhibitor

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