| 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 | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | Ethanol : 10 mg/mL (22.5 mM), Sonication and heating are recommended.
DMSO : 20 mg/mL (45 mM), Sonication and heating are recommended.
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| Keywords | wortmannin | thrombosis | Thrombin receptors | thrombin | SCH-79797 dihydrochloride | SCH79797 dihydrochloride | SCH-79797 | SCH79797 | SCH 79797 Dihydrochloride | SCH 79797 | ProteaseactivatedReceptor | Proteaseactivated Receptor | Protease activated receptor 1 (PAR1) | Protease Activated Receptor (PAR) | pro-apoptotic | platelets | PAR-1 | PAR1 | Nonpeptide | Inhibitor | inhibit | infarct | cardioprotection | Apoptosis | antiproliferative |
| Inhibitors Related | Stavudine | Aceglutamide | Urea | Tamoxifen | Cysteamine hydrochloride | Metronidazole | Citric Acid Triammonium | Formamide | Dimethyl phthalate | Alginic acid | Sodium Molybdate | Sildenafil citrate |
| Related Compound Libraries | Highly Selective Inhibitor Library | Apoptosis Compound Library | Bioactive Compound Library | Membrane Protein-targeted Compound Library | Inhibitor Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Compound Library |
United States
