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)
All
Chemical Reagents
Biomedicine
Organic raw materials
Inorganic chemical industry
intermediate
Agricultural chemicals
Auxiliaries and catalysts
Fragrances and Flavors
Dyes and Pigments
Daily chemical industry
GSK2256294A
CAS number：1142090-23-0(DMSO) molecular formula：C21H24F3N7O
overview
compound introduction
Specs
| Chinese alias | - | ||
| English alias | - | ||
| CAS number | 1142090-23-0(DMSO) | molecular formula | C21H24F3N7O |
| molecular weight | 447.46 g/mol | Exact mass | - |
| PSA | - | logp | - |
numbering system
No numbering system information yet
physicochemical properties
No physical and chemical property information yet
Safety information
No safety information yet
Production methods and uses
No production method and use information yet
Related
upstream information
No upstream information yet
downstream information
No downstream information yet
MSDS
Found 0 shareMSDS
