PF-4693627

PF-4693627 is an orally bioavailable inhibitor of microsomal prostaglandin E (PGE) synthase-1 (mPGES-1, IC50 = 3 nM). It is selective for mPGES-1 over PGDS, TXAS, and 5-LO in HWB-1483 cells, which have IC50 values greater than 50 µM, as well as COX-2 in fetal fibroblasts (IC50 = >10 µM). PF-4693627 inhibits LPS-stimulated synthesis of PGE2 in human whole blood (IC50 = 109 nM). In vivo, PF-4693627 (10 mg/kg) inhibits PGE2 production in a guinea pig model of carrageenan-induced air pouch inflammation.Formal Name: 1-[5-chloro-6-(4-chlorophenyl)-2-benzoxazolyl]-N-[(1S,3S)-3-(hydroxymethyl)cyclohexyl]-4-piperidinecarboxamide. CAS Number: 1312815-93-2. Molecular Formula: C26H29Cl2N3O3. Formula Weight: 502.4. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 10 mg/ml, DMSO: 10 mg/ml, DMSO:PBS (pH 7.2) (1:2): 0.33 mg/ml, Ethanol: 5 mg/ml. lambdamax: 300 nm. SMILES: ClC1=CC=C(C2=CC(OC(N3CCC(C(N[C@@H]4C[C@@H](CO)CCC4)=O)CC3)=N5)=C5C=C2Cl)C=C1. InChi Code: InChI=1S/C26H29Cl2N3O3/c27-19-6-4-17(5-7-19)21-13-24-23(14-22(21)28)30-26(34-24)31-10-8-18(9-11-31)25(33)29-20-3-1-2-16(12-20)15-32/h4-7,13-14,16,18,20,32H,1-3,8-12,15H2,(H,29,33)/t16-,20-/m0/s1. InChi Key: CPDNPVKDQXLYHO-JXFKEZNVSA-N.