AY77 is a calcium-biased PAR2 agonist. AY77 shows an EC50 of 0.17 and 2 nM in PAR2-mediated the activation in the Gq pathway and recruitment of β-arrestin-2, respectively. AY77 potently induces intracellular Ca2+ release.
References:
[1]. Klösel I, et al. Discovery of Novel Nonpeptidic PAR2 Ligands. ACS Med Chem Lett. 2020 May 22;11(6):1316-1323.
[2]. Jiang Y, et al. Biased Signaling by Agonists of Protease Activated Receptor 2. ACS Chem Biol. 2017 May 19;12(5):1217-1226.
















