PAR2 antagonist C781 is a potent β-Arrestin biased protease-activated receptor-2 (PAR2) antagonist, effectively reduces 2AT, trypsin and elastase-induced signalling in vitro physiological assays.
C781 antagonizes PAR2 signalling following peptidomimetic and proteinase-mediated receptor activation in cells naturally expressing the human PAR2 receptor.
C781 effectively reduces 2AT-induced (600 nM) MAPK phosphorylation in a concentration-dependent fashion with significant inhibitory effects using signalling-specific assays in 16HBE14o- cells, with no effect on the Gq/Ca2+ signalling pathway.
C781 reduces airway hyperresponsiveness, limits acute A. alternata-induced inflammation in an acute A. alternata exposure model.
C781 limits acute A. alternata-induced production of inflammatory cytokines, shows limited effect on acute A. alternata-induced airway epithelial mucin expression.