AZ 3451 CAS NO.2100284-59-9

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AZ3451 is a potent and selective allosteric antagonist of protease-activated receptor 2 (PAR2) with IC50 of 23 nM. AZ3451 was found to bind to a remote allosteric site outside the helical bundle that is different from the site previously found on PAR1. The interaction of AZ3451 with PAR2 is predominately hydrophobic in nature. AZ3451 binds to a remote allosteric site outside the helical bundle, which prevents structural rearrangements required for receptor activation and signaling.