BGC-20-1531-(hydro-chloride)

BGC 20-1531 is a potent and selective antagonist of the prostaglandin E2 (PGE2; Item No. 14010) receptor subtype 4 (EP4) with Ki values of 11.7, >10,000, and >10,000 nM for EP4, EP2, and EP3, respectively. It is selective for EP4, exhibiting <50% inhibition at 47 ion channels, cell-surface transporters, enzymes, and nuclear receptors at a concentration of 10 μM. BGC 20-1531 antagonizes PGE2-induced cAMP accumulation in a dose-dependent manner in HEK293 EBNA cells that stably express human EP4 receptors. It also reverses PGE2-induced vasorelaxation (Kb = 15.85 nM) in human middle cerebral and middle...