ASP7657

ASP7657 is a potent and selective small molecule antagonist of the prostaglandin E2 (PGE2) receptor subtype EP4. It exhibits high affinity for both human and rat EP4 receptors, with Kis of 2.21 nM and 6.02 nM, respectively. ASP7657 selectively inhibits PGE2-induced cAMP accumulation in cells expressing EP4 receptors but does not significantly affect other prostaglandin E receptor subtypes (EP1, EP2, or EP3) or a broad panel of other receptors and ion channels. In preclinical studies, oral administration of ASP7657 demonstrated pharmacological activity by antagonizing PGE2-mediated effects such as inhibition of lipopolysaccharide-induced TNF-α release and reducing albuminuria in type 2 diabetic mice models, suggesting potential utility in nephropathy associated with diabetes[1][3][5]. The compound has been evaluated for safety, tolerability, pharmacokinetics, and pharmacodynamics in healthy volunteers[4]. It is primarily developed as a research tool to clarify the physiological and pathophysiological roles of the EP4 receptor.

Other names

ASP7657 mesylateASP-7657 mesylateASP 7657 mesylate