2100284-59-9

AZ3451 has been used as a protease-activated receptor 2 (PAR-2) antagonist to study the involvement of PAR-2 receptors in factor X activated (FXa)-induced upregulation of the cell adhesion molecules.

ChEBI: AZ3451 is a member of the class of benzimidazoles that is 1H-benzimidazole substituted by (1S)-1-cyclohexylethyl, 6-bromo-1,3-benzodioxol-5-yl, and 4-(cyanoanilino)acyl groups at positions 1, 2 and 5, respectively. It is an allosteric modulator of protease-activated receptor 2 (IC50 = 23 nM) and exhibits anti-osteoarthritis properties. It has a role as an anti-inflammatory agent, a PAR2 negative allosteric modulator and an autophagy inducer. It is a secondary carboxamide, a nitrile, a member of benzimidazoles, a member of benzodioxoles and an organobromine compound.

AZ3451 is a potent protease-activated receptor 2 (PAR2) antagonist that binds to a distant allosteric site outside the helical bundle with an IC50 of 23 nM.

Target	Value
PAR2 (Cell-free assay)	23 nM

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