| 产品描述： | 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 |
| 靶点： |
IC50: 27 pM (recombinant human sEH), 61 pM (rat sEH orthologs), 189 pM (murine sEH orthologs);Others; EpoxideHydrolase |
| 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. |
| 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. |
| 参考文献： |
1. Podolin PL, Bolognese BJ, Foley JF, Long E 3rd, Peck B, Umbrecht S, Zhang X,Zhu P, Schwartz B, Xie W, Quinn C, Qi H, Sweitzer S, Chen S, Galop M, Ding Y,Belyanskaya SL, Israel DI, Morgan BA, Behm DJ, Marino JP Jr, Kurali E, BarnetteMS, Mayer RJ, Booth-Genthe CL, Callahan JF. In vitro and in vivo characterizationof a novel soluble epoxide hydrolase inhibitor. Prostaglandins Other LipidMediat. 2013 Jul-Aug;104-105:25-31. doi: 10.1016/j.prostaglandins.2013.02.001.Epub 2013 Feb 19. PubMed PMID: 23434473. |
| 溶解性： |
soluble in DMSO |
| 保存条件： |
-20℃ |
| 配置溶液浓度参考： |
|
1mg |
5mg |
10mg |
| 1 mM |
2.235 ml |
11.174 ml |
22.349 ml |
| 5 mM |
0.447 ml |
2.235 ml |
4.47 ml |
| 10 mM |
0.223 ml |
1.117 ml |
2.235 ml |
| 50 mM |
0.045 ml |
0.223 ml |
0.447 ml |
|
| 注意： |
部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京