CAY10598

Prostaglandin E2 (PGE2) activates four E prostanoid (EP) receptors, EP1-4. EP4 is a Gs protein-coupled receptor that, by elevating the second messenger cAMP, plays important roles in bone formation and resorption, cancer, and atherosclerosis.{16772,16773,16619} CAY10598 is a very potent agonist of EP4, binding with a Ki value of 1.2 nM.{16762} Moreover, it does not bind EP1, EP2, EP3, or other prostanoid receptors, including DP, FP, IP, and TP.{16762} First generation EP4 receptor-selective agonists have been shown to reduce inflammation, improve bone healing, provide cardio- and neuroprotection, and reduce renal dysfunction, suggesting some clinical applications for EP4 agonists.{18099,18101,18100,18103,18102}