Name | SCH79797 dihydrochloride |
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]. |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | Ethanol : 10 mg/mL (22.50 mM), Sonication and heating are recommended. DMSO : 20 mg/mL (45.00 mM), Sonication and heating are recommended.
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Keywords | infarct | SCH79797 dihydrochloride | SCH-79797 | SCH-79797 dihydrochloride | SCH 79797 | Inhibitor | inhibit | Nonpeptide | SCH79797 | SCH79797 Dihydrochloride | thrombin | wortmannin | antiproliferative | platelets | Protease Activated Receptor (PAR) | SCH 79797 Dihydrochloride | pro-apoptotic | thrombosis | SCH-79797 Dihydrochloride | Thrombin receptors | PAR1 | cardioprotection | Apoptosis |
Inhibitors Related | Stavudine | 5-Fluorouracil | Acetylcysteine | Kaempferol | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Metronidazole | Sorafenib | Tributyrin | Lidocaine hydrochloride |
Related Compound Libraries | Highly Selective Inhibitor Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library |