Cayman CJ-42794

Prostaglandin E₂ (PGE₂) activates four E prostanoid (EP) receptors, EP_1-4. 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.^1,2,3 CJ-42794 is a selective antagonist of EP₄ (K_i = 3.16 nM) that less potently binds EP₂ (K_i = 631 nM) and has no affinity for EP₁ or EP₃.^4,5 It has minimal effect on numerous other receptors, enzymes, or channels.⁵ Unlike general inhibitors of PGE₂ synthesis, CJ-42794 does not cause damage to rat gastrointestinal mucosa.⁴ Instead, it delays the healing of gastric ulcers in mice and rats, suppressing the upregulation of VEGF expression and angiogenesis.⁶ CJ-42794 blocks pain and inflammation in rat models of arthritis as well as gastric tumorigenesis in mice.^7,8

WARNING This product is not for human or veterinary use.