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. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
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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