GSK2256294A (Synonyms: GSK 2256294)
目录号: PL04915 纯度: ≥99%
CAS No. :1142090-23-0
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中文名称
GSK2256294A
英文名称
GSK2256294A
英文别名
GSK2256294A;(1R,3S)-N-[[4-cyano-2-(trifluoromethyl)phenyl]methyl]-3-[[4-methyl-6-(methylamino)-1,3,5-triazin-2-yl]amino]cyclohexane-1-carboxamide;GSK 2256294;GSK-2256294;GSK-2256294A
Cas No.
1142090-23-0
分子式
C21H24N7OF3
分子量
447.46
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
GSK2256294A (GSK 2256294) 是一种选择性的,以及口服活性的 soluble epoxide hydrolase (sEH) 抑制剂。GSK2256294A 对人的重组 sEH、大鼠同源 sEH 和小鼠同源 sEH 具有抑制作用,其 IC50 值分别为 27、61 和 189 pM。GSK2256294A 可用于慢性阻塞性肺疾病 (COPD) 和心血管疾病的研究。
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 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 disease.
性状
Solid
IC50 & Target[1][2]
IC50: 27 pM (recombinant human sEH), 61 pM (rat sEH orthologs), 189 pM (murine sEH orthologs)
体外研究(In Vitro)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
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. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. Podolin PL, et al. In vitro and in vivo characterization of a novel soluble epoxide hydrolase inhibitor. Prostaglandins Other Lipid Mediat. 2013 Jul-Aug;104-105:25-31.
溶解度数据
In Vitro: DMSO : ≥ 47 mg/mL (105.04 mM)配制储备液
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1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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