GSK2256294A (C09-1135-884)

GSK2256294A (GSK 2256294) is a selective and orally active inhibitor of soluble epoxide hydrolase (sEH) . GSK2256294A inhibits recombinant human sEH, rat sEH orthologs and murine sEH orthologs with IC 50 s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular diseaseIn VitroGSK2256294A (300 pM-10 μM; 2 h) inhibits the conversion of 14,15-EET-d11 to 14,15-DHET-d11 in human, rat and mouse whole blood. MCE has not independently confirmed the accuracy of these methods. They are for reference only.In VivoGSK2256294A (5-30 mg/kg; p.o. twice daily 5 days/week for two weeks) inhibits the generation and maintenance of pulmonary inflammation in cigarette smoke-exposed mice . GSK2256294A (30 mg/kg; p.o. twice daily for 8 days) decreases pulmonary inflammation in cigarette smoke-exposed mice . MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Mice exposed to cigarette smoke 5 days/week for 2 weeks Dosage: 5 and 30 mg/kg Administration: Oral gavage; 5 and 30 mg/kg twice daily 5 days/week; for 2 weeks Result: Dose-dependently inhibited numbers of BAL fluid total cells, neutrophils, macrophages and the keratinocyte chemoattractant (KC) levels in lung tissue. Animal Model: Mice exposed to cigarette smoke 5 days/week for 2 weeks Dosage: 30 mg/kg Administration: Oral gavage; 30 mg/kg twice daily; for 8 days Result: Significantly reduced neutrophils, macrophages and pulmonary inflammation in cigarette smoke-exposed mice.IC50& Target:IC50: 27 pM (recombinant human sEH), 61 pM (rat sEH orthologs), 189 pM (murine sEH orthologs). Specification: 10mM in DMSO Molecular Formula: C21H24F3N7O Molecular Weight: 447.46