ER-819762 is a novel potent, selective, orally active EP4 receptor antagonist with IC50 of 59 nM in cAMP-dependent reporter assay.
ER-819762 inhibits EP4-stimulated Th1 differentiation, Th17 cell expansion, and IL-23 secretion by activated dendritic cells.
ER-819762 exhibits no agonism or antagonism for the related PGE2 EP1, EP2 and EP3 receptors.
ER-819762 suppresses Th1 and Th17 cytokine production, suppresses disease in collagen- and GPI-induced arthritis in mice, and suppresses CFA-induced inflammatory pain in rats.
