PF-04418948

PF-04418948 is an orally active, potent, and selective antagonist of the prostaglandin E2 receptor EP2 (EP2 receptor). It exhibits high selectivity for the EP2 receptor with an IC50 of approximately 16 nM and is over a thousand-fold less active at other prostanoid receptors. Mechanistically, it blocks the action of prostaglandin E2 (PGE2) at the EP2 receptor, which is a G protein-coupled receptor signaling primarily through Gs proteins to increase cAMP. The compound has been used as a tool in preclinical studies to elucidate EP2 function in various tissues including human myometrium, dog bronchiole, and mouse trachea. In vivo studies have shown that oral administration attenuates PGE2-induced physiological responses such as airway microvascular leak and gut dysmotility in animal models. Developed by Pfizer, PF-04418948 reached Phase I clinical trials for safety evaluation in healthy volunteers[1][4][5][6][7].

Other names

1078166-57-0UNII-I7Z38E70VFUNII-I-7Z38E70VFUNII-I 7Z38E70VF