Chemical Name: 2-(6-Bromo-1,3-benzodioxol-5-yl)-N-(4-cyanophenyl)-1-[(1S)-1-cyclohexylethyl]-1H-benzimidazole-5-carboxamide
Biological ActivityAZ 3451 is a potent negative allosteric modulator of PAR2 (IC50 = 23 nM); binds to a remote allosteric site outside the helical bundle. Inhibits ERK phosphorylation in 1321N1 cells overexpressing wild-type human PAR2. Highly lipophilic.
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Tocris products are intended for laboratory research use only, unless stated otherwise.
Structural insight into allosteric modulation of protease-activated receptor 2.
Cheng et al.
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