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Submit ReviewPAR1 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.
分子量 | 369.29 |
公式 | C21H17ClN2.HCl |
储存 | Store at +4°C |
纯度 | ≥99% (HPLC) |
CAS Number | 1052076-77-3 |
PubChem ID | 16258217 |
InChI Key | WXIWQTVPWYFEHP-UHFFFAOYSA-N |
Smiles | ClC(C=C4)=CC=C4CN2C1=CC=CC=C1N=C2CC3=CC=CC=C3.Cl |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
参考文献是支持产品生物活性的出版物。
Deng et 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
Asteriti et al (2012) Modulation of PAR1 signalling by benzimidazole compounds. Br.J.Pharmacol. 167 80 PMID: 22519452
Scotton et 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
关键词: Q94 hydrochloride, Q94 hydrochloride supplier, PAR1, protease, activated, receptors, negative, allosteric, modulators, selective, blocks, thrombin, induced, calcium, mobilization, NAM, Protease-Activated, Receptors, 4755, Tocris Bioscience
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