Description: PF-04418948 is a potent EP2 receptor antagonist (IC50 = 16 nM for human EP2 receptors). Displays over 2000-fold selectivity for EP2 receptors over EP1, EP3, EP4, DP1 amd CRTH2 receptors, exhibits <30% binding at a diverse panel of GPCRs and ion channels at a concentration of 10 µM. Inhibits PGE2-induced...

Prostaglandin E2 (PGE2) evokes distinct responses through four different 'E prostanoid' (EP) receptors. EP2 is a G protein-coupled receptor which signals preferentially through Gs proteins. PF-04418948 is an orally active, potent, and selective EP2 receptor antagonist (IC50 = 16 nM). It is over a thousand-fold less...