SCH79797 dihydrochloride  ≥98%

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包装规格:1mg 5mg 10mg 25mg 50mg 100mg in glass bottle
溶解性:溶于DMSO(22 mg/mL 超声,加热)
产品描述:基本信息 产品编号: S10692  产品名称: SCH79797 dihydrochloride CAS: 1216720-69-2   储存条件 粉末 -20℃ 四年     分子式: C23H27Cl2N5 溶于液体 -80℃ 6个月 分子量: 444.40 -20℃ 1个月 化学名:  N3-环丙基-7-[[4-(1-甲基乙基)苯基]甲基]-7H-吡咯并[3,2-f]喹唑啉-1,3-二胺双盐酸盐N3-Cyclopropyl-7-[[4-(1-methylethyl)phenyl]methyl]-7H-pyrrolo[3,2-f]quinazoline-1,3-diamine Dihydroc Solubility (25°C):   体外:   DMSO   Ethanol   Water   体内(现配现用):   <1mg/ml表示微溶或不溶。 普西唐提供的所有化合物浓度为内部测试所得,实际溶液度可能与公布值有所偏差,属于正常的批间细微差异现象。 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;⼀旦配成溶液,请分装保存,避免反复冻融造成的产品失效。   生物活性 产品描述 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 70nM,Ki 为 35nM。 靶点 Protease-Activated Receptor (PAR) Apoptosis   体外研究 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 75nM,81nM 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. 体内研究 SCH79797 (2.5-250μg/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 25μg/kg. Animal Model: Male Sprague Dawley rats (8 weeks of age) with myocardial I/R injury. Dosage: 2.5μg/kg,10μg/kg,25μg/kg,50μg/kg,100μg/kg,and 250μg/kg Administration: Intravenous injection Result: Immediately before or during ischemia reduced myocardial necrosis following I/R in the intact rat heart.
保存条件:-20℃