货号 | 4755/50 |
别名 | 1-[(4-Chlorophenyl)methyl]-2-(pheny |
供应商 | Tocris |
生物活性 | PAR1 negative allosteric modulator (IC50 = 916 nM); inhibits PAR1-Gαq interaction. Selective for PAR1 over PAR2. Blocks thrombin-induced intracellular calcium mobilization (IC50 = 10.3 nM), CCL2 expression, ERK1/2 and MLC phosphorylation, and IP3 production in cells. |
运输条件 | Blue Ice |
存放说明 | 4℃ |
纯度 | >99 % |
计算分子量 | 369.29 |
分子式 | C21H17ClN2.HCl |
可溶性/溶解性 | Soluble to 50 mM in DMSO and to 50 mM in ethanol |
参考文献 | Asteritiet al (2012) Modulation of PAR1 signalling by benzimidazole compounds. Br.J.Pharmacol. 167 80. PMID: 22519452. Scottonet al (2009) Increased local expression of coagulation factor X contributes to the fibrotic response in human and murine lung injury. J.Clin.Invest. 119 2550. PMID: 19652365. Denget al (2008) Thrombin induces fibroblast CCL2/JE production and release via coupling of PAR1 to Gαq and cooperation between ERK1/2 and Rho kinase signaling pathways. Mol.Biol.Cell 19 2520. PMID: 18353977. |