Chemical Name: 1-[(4-Chlorophenyl)methyl]-2-(phenylmethyl)-1H-benzimidazole hydrochloride
Biological ActivityPAR1 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.
The technical data provided above is for guidance only.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Thrombin induces fibroblast CCL2/JE production and release via coupling of PAR1 to Gαq and cooperation between ERK1/2 and Rho kinase signaling pathways.
Deng et al.
Modulation of PAR1 signalling by benzimidazole compounds.
Asteriti et al.
Increased local expression of coagulation factor X contributes to the fibrotic response in human and murine lung injury.
Scotton et al.
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