A Gαq-signaling-biased PAR1 antagonist
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Q94 (hydrochloride hydrate)

Item No. 32857

Technical Information
Formal Name
1-[(4-chlorophenyl)methyl]-2-(phenylmethyl)-1H-benzimidazole, monohydrochloride, hydrate
Molecular Formula
C21H17ClN2 • HCl [XH2O]
Formula Weight
Purity
≥98%
Formulation
A solid
DMSO: 30 mg/ml
SMILES
ClC1=CC=C(CN2C3=C(N=C2CC4=CC=CC=C4)C=CC=C3)C=C1.Cl.O
InChi Code
InChI=1S/C21H17ClN2.ClH.H2O/c22-18-12-10-17(11-13-18)15-24-20-9-5-4-8-19(20)23-21(24)14-16-6-2-1-3-7-16;;/h1-13H,14-15H2;1H;1H2
InChi Key
FOPYUSPZJBXRMQ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    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

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Asteriti, S., Daniele, S., Porchia, F., et alModulation of PAR1 signalling by benzimidazole compounds. Br. J. Pharmacol. 167(1), 80-94 (2012).

    2. Deng, X., Mercer, P.F., Scotton, C.J., et alThrombin 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. Guan, Y., Nakano, D., Zhang, Y., et alA protease-activated receptor-1 antagonist protects against podocyte injury in a mouse model of nephropathy. J. Pharmacol. Sci. 135(2), 81-88 (2017).