产品描述:
Prostaglandin E2 (PGE2; Item No. 14010) 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, inflammation, cancer, and atherosclerosis.{16772,16773,16619} MF498 is a selective EP4 receptor antagonist (Ki = 0.7 nM versus a Ki > 1 µM for other EP receptors).{18105} In HEK293 cells expressing the human EP4 receptor, MF498 inhibits EP ligand induced activity with an IC50 value of 1.7 nM.{18105} In various animal models for arthritis, MF498 has been shown to inhibit inflammation without gastrointestinal toxicity (ED50 values as low as 0.02 mg/kg/day).{18105}