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编 号:F044543
分子式:C21H24F3N7O
分子量:447.46
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10mM*1mL in DMSO
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1mg
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5mg
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10mg
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50mg
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生物活性:
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 IC50s of 27, 61 and 189 pM, respectively. GSK2256294A can be used for the research of chronic obstructive pulmonary disease (COPD) and cardiovascular disease.

体内研究:
GSK2256294A (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.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.

体外研究:
GSK2256294A (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.
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