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SCH79797 dihydrochloride

CAS No. : 1216720-69-2

MCE 国际站：SCH79797 dihydrochloride

产品活性：SCH79797 dihydrochloride 是一种高效的选择性非肽蛋白酶激活受体 1 (PAR1) 拮抗剂。SCH79797 dihydrochloride 抑制高亲和力的凝血酶受体激活肽与 PAR1 的结合，IC₅₀ 值为 70 nM，K_i 为 35 nM。SCH79797 dihydrochloride 以 IC₅₀ 为 3 μM 抑制凝血酶诱导的血小板凝集。SCH79797 dihydrochloride 具有抗增殖和促凋亡作用，并限制了大鼠心脏的心肌缺血/再灌注损伤。SCH79797 dihydrochloride 还可以有效地阻止血管平滑肌细胞，内皮细胞和星形胶质细胞中的 PAR1 活化。

研究领域：GPCR/G Protein  |  Apoptosis

作用靶点：Protease Activated Receptor (PAR)  |  Apoptosis

In Vitro: SCH79797 inhibits high-affinity thrombin receptor-activating peptide ([³H]haTRAP) binding in a competitive manner. SCH79797 inhibits α-thrombin- and haTRAP-induced aggregation of human platelets, but does not inhibit human platelet aggregation induced by the tethered ligand agonist for protease-activated receptor-4 (PAR-4), γ-thrombin, ADP, or collagen. Thrombin produces transient increases in cytosolic free Ca²⁺ concentration ([Ca²⁺]_i) in hCASMC. SCH79797 effectively inhibits this increase in [Ca²⁺]_i. SCH79797 completely inhibits Thrombin- and TK-stimulated [³H]thymidine incorporation .
SCH79797 is able to interfere with the growth of several human and mouse cell lines, in a concentration-dependent manner. The ED₅₀ for growth inhibition iss 75 nM, 81 nM and 116 nM for NIH 3T3, HEK 293 and A375 cells, respectively. In NIH 3T3 cells, SCH79797 inhibits serum-stimulated activation of p44/p42 mitogen-activated protein kinases (MAPK) at low concentrations and induces apoptosis at higher concentrations.

In Vivo: SCH79797 (2.5-250 μg/kg; intravenous injection; male Sprague Dawley rats) treatment immediately before or during ischemia reduces myocardial necrosis following I/R in the intact rat heart in two rat models of myocardial ischemia/reperfusion (I/R) injury. This response is dose-dependent with the optimal dose being 25 μg/kg.

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