PF-9184

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product prostaglandin H2 (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. PF-9184 is a potent inhibitor of mPGES-1 (IC50 = 16.5 nM for recombinant human enzyme). It displays at least 6,500-fold selectivity for mPGES-1 over COX-1 and COX-2. PF-9184 blocks the synthesis of PGE2 in LPS-treated human whole blood and in IL-1beta-stimulated fibroblasts (IC50s = 0.4-5 µM).Formal Name: N-(3',4'-dichloro[1,1'-biphenyl]-4-yl)-4-hydroxy-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxide. CAS Number: 1221971-47-6. Molecular Formula: C21H14Cl2N2O4S. Formula Weight: 461.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 20 mg/ml, DMSO: 15 mg/ml. lambdamax: 269, 335 nm. SMILES: OC1=C(C(NC2=CC=C(C3=CC=C(Cl)C(Cl)=C3)C=C2)=O)NS(C4=CC=CC=C41)(=O)=O. InChi Code: InChI=1S/C21H14Cl2N2O4S/c22-16-10-7-13(11-17(16)23)12-5-8-14(9-6-12)24-21(27)19-20(26)15-3-1-2-4-18(15)30(28,29)25-19/h1-11,25-26H,(H,24,27). InChi Key: VGACSWBJQLLJFB-UHFFFAOYSA-N.