MCE 的所有产品仅用作科学研究，我们不为任何个人用途提供产品和服务。

SCH79797 dihydrochloride

CAS No. : 1216720-69-2

MCE 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.

相关产品：MG-132  |  LY294002  |  Actinomycin D  |  Mitomycin C  |  Doxorubicin hydrochloride  |  Bafilomycin A1  |  Paclitaxel  |  Y-27632 dihydrochloride  |  SP600125  |  Sorafenib  |  Angiotensin II human  |  MK-2206 dihydrochloride  |  5-Fluorouracil  |  Trametinib  |  Tamoxifen  |  Bortezomib  |  Gemcitabine  |  Pexidartinib  |  Acetylcysteine  |  Decitabine  |  BAY 11-7082  |  2-Deoxy-D-glucose  |  Docetaxel  |  Verteporfin  |  Temozolomide  |  Dasatinib  |  Ruxolitinib  |  Etoposide  |  DAPT

品牌介绍:
•   MCE (MedChemExpress) 拥有数百种全球独家化合物，我们致力于为全球科研客户提供*新*全的高品质小分子活性化合物；
•   10,000 多种高选择性抑制剂、激动剂涉及各热门信号通路及疾病领域；
•   设有专业的实验中心和严格的质控、验证体系；
•   提供 LC/MS、NMR、HPLC、手性分析、元素分析等各项质检报告，确保产品的高纯度、高品质；
•   产品的生物活性多经各国客户实验验证；
•   Nature, Cell, Science 等多种期刊及制药收录了MCE客户的科研成果；
•   专业团队跟踪*新的制药及生命科学研究进展，为您提供全球*新的活性化合物；
•   与世界各大制药公司及知名科研机构建立了长期的合作。