GSK2256294A

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GSK2256294A 是重组人、大鼠和小鼠 sEH 的有效选择性抑制剂，IC50 分别为 27 pM、61 pM 和 189 pM。

GSK2256294A is potent, selective inhibitor of recombinant human, rat and mouse sEH with IC50 of 27 pM, 61 pM and 189 pM, respectively.(In Vitro):GSK2256294A displays potent cellular inhibition of sEH with an IC50 of 0.66 nM in an assay developed using a cell line transfected with the human sEH enzyme.(In Vivo):Mice receiving 10 days of cigarette smoke exposure concomitant with oral administration of GSK2256294A exhibits significant, dose-dependent reductions in pulmonary leukocytes and keratinocyte chemoattractant levels. Mice receiving oral administration of GSK2256294A following 10 days of cigarette smoke exposure exhibited significant reductions in pulmonary leukocytes compared to vehicle-treated mice.

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.

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.

GSK 2256294

Others

Other Targets

Bacterial| Human Endogenous Metabolite

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1142090-23-0

447.466

C21H24F3N7O

>98% (HPLC)

In Vitro:?DMSO : ≥ 47 mg/mL (105.04 mM)

CNc1nc(C)nc(N[C@H]2CCC[C@H](C2)C(=O)NCc2ccc(cc2C(F)(F)F)C#N)n1

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(-20℃)

With Ice Pack

≥ 2 years