| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| G655175-1ml |
1ml |
期货  |
|
| 规格或纯度 | Moligand™, 10mM in DMSO |
|---|---|
| 英文名称 | GSK2256294A |
| 生化机理 | GSK2256294A （GSK 2256294）是一种具有选择性和口服活性的可溶性环氧化物水解酶（sEH）抑制剂。GSK2256294A 可抑制重组人 sEH、大鼠 sEH 同源物和小鼠 sEH 同源物，其 IC 50 s 分别为 27、61 和 189 pM。GSK2256294A c |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 作用类型 | 抑制剂 |
| 作用机制 | 环氧化物氢化酶抑制剂 |
| 产品介绍 |
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。
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 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. MCE has not independently confirmed the accuracy of these methods. They are for reference only. 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 . 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) |
| ALogP | 3.7 |
|---|
| 分子类型 | 小分子 |
|---|---|
| Isomeric SMILES | CC1=NC(=NC(=N1)N[C@H]2CCC[C@H](C2)C(=O)NCC3=C(C=C(C=C3)C#N)C(F)(F)F)NC |
| PubChem CID | 59448236 |
| 分子量 | 447.46 |
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