CJ-42794

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. 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. It has minimal effect on numerous other receptors, enzymes, or channels. Unlike general inhibitors of PGE2 synthesis, CJ-42794 does not cause damage to rat gastrointestinal mucosa. Instead, it delays the healing of gastric ulcers in mice and rats, suppressing the upregulation of VEGF expression and angiogenesis. CJ-42794 blocks pain and inflammation in rat models of arthritis as well as gastric tumorigenesis in mice.Formal Name: 4-[(1S)-1-[[5-chloro-2-(4-fluorophenoxy)benzoyl]amino]ethyl]-benzoic acid. CAS Number: 847728-01-2. Synonyms: RQ-00015986. Molecular Formula: C22H17ClFNO4. Formula Weight: 413.8. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2) (1:1): 0.5 mg/ml, DMSO: 25 mg/ml, Ethanol: 25 mg/ml. lambdamax: 234 nm. SMILES: FC1=CC=C(OC2=C(C(N[C@@H](C)C3=CC=C(C(O)=O)C=C3)=O)C=C(Cl)C=C2)C=C1. InChi Code: InChI=1S/C22H17ClFNO4/c1-13(14-2-4-15(5-3-14)22(27)28)25-21(26)19-12-16(23)6-11-20(19)29-18-9-7-17(24)8-10-18/h2-13H,1H3,(H,25,26)(H,27,28)/t13-/m0/s1. InChi Key: MWBNCZHVEXULBD-ZDUSSCGKSA-N.