Q94 hydrochloride

Cat. No. 4755

Q94 hydrochloride C21H17ClN2.HCl [1052076-77-3]

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Chemical Name: 1-[(4-Chlorophenyl)methyl]-2-(phenylmethyl)-1H-benzimidazole hydrochloride

Biological Activity

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.

Technical Data

M.Wt:
369.29
Formula:
C21H17ClN2.HCl
Solubility:
Soluble to 50 mM in DMSO and to 50 mM in ethanol
Purity:
>99 %
Storage:
Store at +4°C
CAS No:
1052076-77-3

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.

Certificate of Analysis / Product Datasheet / Safety Datasheet

References are publications that support the products' biological activity.

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.

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.

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Keywords: Q94 hydrochloride, supplier, PAR1, protease, activated, receptors, negative, allosteric, modulators, selective, blocks, thrombin, induced, calcium, mobilization, Tocris Bioscience, Protease-Activated Receptor Modulator products

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