PF-04418948

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 increases in intracellular cAMP, reverses PGE2-invoked relaxation of mouse trachea (IC50 = 2.7 nM). Target: Prostaglandin Receptor. Smiles: COc1ccc2cc(OCC3(CN(C3)C(=O)c3ccc(F)cc3)C(O)=O)ccc2c1. References: af Forselles KJ, et al. In vitro and in vivo characterization of PF-04418948, a novel, potent and selective prostaglandin EP2 receptor antagonist. Br J Pharmacol. 2011 Dec,164(7):1847-1856