CAY10678

Microsomal prostaglandin E synthase-1 (mPGES-1) converts the COX product PGH2 into the biologically active PGE2. Like COX-2, the expression of mPGES-1 is induced in response to pro-inflammatory mediators, including LPS, IL-1beta, and TNF-alpha. CAY10678 is a benzoimidazole that potently inhibits human and rat recombinant mPGES-1 (IC50 = 0.09 and 0.9 µM, respectively). It has minimal effects on COX-1, COX-2, PGIS, and hematopoietic PGDS at 50 µM but reduces lipocalin-type PGDS activity by 60% at this concentration. CAY10678 dose-dependently blocks PGE2 synthesis in isolated cells and whole blood treated with LPS or IL-1beta. It also dose-dependently reduces PGE2 synthesis and cell recruitment during inflammation in mice.Formal Name: N-cyclopentyl-1-[5,6-dimethyl-1-(1-methylethyl)-1H-benzimidazol-2-yl]-4-piperidinecarboxamide. CAS Number: 1268709-57-4. Synonyms: mPGES-1 Inhibitor III. Molecular Formula: C23H34N4O. Formula Weight: 382.5. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 15 mg/ml, DMSO: 5 mg/ml, Ethanol: 25 mg/ml, Ethanol:PBS (pH 7.2) (1:8): 0.1 mg/ml. lambdamax: 215, 250, 292 nm. SMILES: O=C(C1CCN(C2=NC3=CC(C)=C(C)C=C3N2C(C)C)CC1)NC4CCCC4. InChi Code: InChI=1S/C23H34N4O/c1-15(2)27-21-14-17(4)16(3)13-20(21)25-23(27)26-11-9-18(10-12-26)22(28)24-19-7-5-6-8-19/h13-15,18-19H,5-12H2,1-4H3,(H,24,28). InChi Key: FPPVJOTXZIRXTF-UHFFFAOYSA-N.