SCH79797 dihydrochloride

SKU: orb1309114

Description

SCH79797 dihydrochloride is a potent and selective PAR1 antagonist with a Ki of 35 nM. It exhibits antiproliferative and pro-apoptotic activities, making it a useful tool for studying PAR1's role in cancer, thrombosis, and inflammation in both cellular and animal models.

Research Area

Cell Biology, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	1216720-69-2
MW	444.4
Purity	99.50% (May vary between batches)
Formula	C₂₃H₂₇Cl₂N₅
SMILES	Cl.Cl.CC(C)c1ccc(Cn2ccc3c2ccc2nc(NC4CC4)nc(N)c32)cc1
Target	Apoptosis,Protease-activated Receptor
Solubility	Ethanol:10 mg/mL (22.5 mM);DMSO:20 mg/mL (45 mM)

Bioactivity

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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.

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. 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 .

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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cardioprotection, Apoptosis, antiproliferative, Inhibitor, Nonpeptide, inhibit, infarct, platelets, PAR-1, PAR1, thrombin, Thrombin receptors, thrombosis, pro-apoptotic, wortmannin, SCH 79797, SCH 79797 Dihydrochloride, SCH79797, SCH-79797, SCH79797 dihydrochloride, SCH79797 Dihydrochloride, SCH-79797 dihydrochloride, SCH-79797 Dihydrochloride, ProteaseactivatedReceptor, Protease activated receptor 1 (PAR1), Proteaseactivated Receptor, Protease Activated Receptor (PAR)

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Compound Identifiers

PubChem CID

45073452 ↗

Key Properties

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No computed properties available.

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