产品描述:
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} CJ-42794 is a selective antagonist of EP4 (Ki = 3.16 nM) that less potently binds EP2 (Ki = 631 nM) and has no affinity for EP1 or EP3.{14996,26030} It has minimal effect on numerous other receptors, enzymes, or channels.{26030} Unlike general inhibitors of PGE2 synthesis, CJ-42794 does not cause damage to rat gastrointestinal mucosa.{14996} Instead, it delays the healing of gastric ulcers in mice and rats, suppressing the upregulation of VEGF expression and angiogenesis.{26032} CJ-42794 blocks pain and inflammation in rat models of arthritis as well as gastric tumorigenesis in mice.{25895,26031}