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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.
|Storage||Store at +4°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
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 the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|0.5 mM||5.42 mL||27.08 mL||54.16 mL|
|2.5 mM||1.08 mL||5.42 mL||10.83 mL|
|5 mM||0.54 mL||2.71 mL||5.42 mL|
|25 mM||0.11 mL||0.54 mL||1.08 mL|
References are publications that support the biological activity of the product.
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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