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Q94 is a Gαq signaling-biased antagonist of proteinase-activated receptor 1 (PAR1; IC50 = 916 nM).1,2 It inhibits increases in intracellular calcium mobilization induced by thrombin or a PAR1-activating peptide, but not a PAR2-activating peptide, in HMEC-1 cells when used at concentrations of 1 and 10 μM.1 Q94 (5 mg/kg per day) decreases albuminuria in a mouse model of nephropathy induced by doxorubicin (Item No. 15007).3
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1. Modulation of PAR1 signalling by benzimidazole compounds. Br. J. Pharmacol. 167(1), 80-94 (2012).
2. 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(6), 2520-2533 (2008).
3. A protease-