AF3485

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 (Cay-17020) into the biologically active PGE2 (Cay-14010). Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1beta, and TNF-alpha. AF3485 is a selective 3-aminocarbazole inhibitor of mPGES-1, blocking the synthesis of PGE2 but not PGF2alpha (Cay-16010) in A549 cells stimulated with IL-1beta (IC50s = 2.9 and >100 µM, respectively). It reduces inflammatory pain (acetic acid-induced writhing) in mice by 74% when given intraperitoneally at 10 mg/kg. AF3485 is absorbed through enterocytes, is metabolically stable in human and rat microsome preparations, and is bioavailable in vivo.Formal Name: N-[9-(2-hydroxyethyl)-9H-carbazol-3-yl]-2-(trifluoromethyl)-benzamide. CAS Number: 1195786-61-8. Synonyms: CAY10686. Molecular Formula: C22H17F3N2O2. Formula Weight: 398.4. Purity: >95%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMF:PBS (pH 7.2), (1:7): 0.1 mg/ml, DMSO: 10 mg/ml, Ethanol: 0.3 mg/ml. lambdamax: 240, 281, 350 nm. SMILES: OCCN(C1=C2C=CC=C1)C3=C2C=C(NC(C4=CC=CC=C4C(F)(F)F)=O)C=C3. InChi Code: InChI=1S/C22H17F3N2O2/c23-22(24,25)18-7-3-1-6-16(18)21(29)26-14-9-10-20-17(13-14)15-5-2-4-8-19(15)27(20)11-12-28/h1-10,13,28H,11-12H2,(H,26,29). InChi Key: RXVOFPXZHVKZIL-UHFFFAOYSA-N.