Vipoglanstat

Vipoglanstat is an inhibitor of microsomal prostaglandin E synthase-1 (mPGES-1, IC50 = =0.5 nM in isolated human whole blood). It reduces LPS-induced increases in the influx of neutrophils and levels of cytokines in bronchoalveolar lavage fluid (BALF), as well as the expression of PTGES, the gene encoding mPGES-1, Cox2, and Icam1 in the lung parenchyma, in a human PTGES knock-in mouse model of acute lung injury when administered at a dose of 30 mg/kg. Vipoglanstat (30 mg/kg) also reduces the lung injury score and expression of PTGES and Nos2, the gene encoding inducible nitric oxide synthase (iNOS), as well as increases survival, in a human PTGES knock-in mouse model of sepsis induced by cecal ligation and puncture. It reduces status epilepticus-induced increases in brain capillary mPGES-1 and P-glycoprotein levels in a human PTGES knock-in mouse model of kainic acid-induced status epilepticus when administered at doses of 10, 30, and 100 mg/kg.Formal Name: 2-[[2,6-dichloro-3-[[(2,2-dimethyl-1-oxopropyl)amino]methyl]phenyl]amino]-6-(2,2-difluoroethoxy)-1-methyl-N-[trans-4-(trifluoromethyl)cyclohexyl]-1H-benzimidazole-5-carboxamide. CAS Number: 1360622-01-0. Synonyms: BI 1029539, GS-248, OX-MPI. Molecular Formula: C30H34Cl2F5N5O3. Formula Weight: 678.5. Purity: >98%. Formulation: (Request formulation change), A solid. Solubility: Acetonitrile: Slightly soluble: 0.1-1 mg/ml, DMSO: Sparingly soluble: 1-10 mg/ml. SMILES: ClC1=CC=C(C(Cl)=C1NC2=NC3=CC(C(N[C@H]4CC[C@H](C(F)(F)F)CC4)=O)=C(OCC(F)F)C=C3N2C)CNC(C(C)(C)C)=O. InChi Code: InChI=1S/C30H34Cl2F5N5O3/c1-29(2,3)27(44)38-13-15-5-10-19(31)25(24(15)32)41-28-40-20-11-18(22(45-14-23(33)34)12-21(20)42(28)4)26(43)39-17-8-6-16(7-9-17)30(35,36)37/h5,10-12,16-17,23H,6-9,13-14H2,1-4H3,(H,38,44)(H,39,43)(H,40,41)/t16-,17-. InChi Key: PFORUFFGGNOLPJ-QAQDUYKDSA-N.