Q94 hydrochloride

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Cat.No. 4755 - Q94 hydrochloride | C21H17ClN2.HCl | CAS No. 1052076-77-3
Description: Negative allosteric modulator at PAR1 receptor
Chemical Name: 1-[(4-Chlorophenyl)methyl]-2-(phenylmethyl)-1H-benzimidazole hydrochloride
Purity: ≥99% (HPLC)
Datasheet
Citations
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Literature

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
Storage Store at +4°C
Purity ≥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

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.

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 18.46 50
ethanol 18.46 50

Preparing Stock Solutions

The following data is based on the product molecular weight 369.29. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.71 mL 13.54 mL 27.08 mL
5 mM 0.54 mL 2.71 mL 5.42 mL
10 mM 0.27 mL 1.35 mL 2.71 mL
50 mM 0.05 mL 0.27 mL 0.54 mL

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Product Datasheets

Safety Datasheet

References

References are publications that support the products' biological activity.

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


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