FRESELESTAT
| 中文名称 | FRESELESTAT |
|---|---|
| 中文同义词 | 夫瑞司他 ONO6818;化合物 T31877 |
| 英文名称 | FRESELESTAT |
| 英文同义词 | FRESELESTAT;1(6H)-PyriMidineacetaMide,5-aMino-N-[1-[[5-(1,1-diMethylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]-2-Methylpropyl]-6-oxo-2-phenyl-;ONO 6818;ONO6818;ONO-6818;ONO-PO-736;5-Amino-N-[1-[[5-(1,1-dimethylethyl)-1,3,4-oxadiazol-2-yl]carbonyl]-2-methylpropyl]-6-oxo-2-phenyl-1(6H)-pyrimidineacetamide;Freselesat |
| CAS号 | 208848-19-5 |
| 分子式 | C23H28N6O4 |
| 分子量 | 452.51 |
| EINECS号 | |
| 相关类别 | |
| Mol文件 | 208848-19-5.mol |
| 结构式 |  |
FRESELESTAT 性质
| 熔点 | 151-153oC |
|---|---|
| 密度 | 1.32±0.1 g/cm3(Predicted) |
| 储存条件 | -20°C Freezer |
| 溶解度 | 可溶于DMSO（少许）、甲醇（少许） |
| 酸度系数(pKa) | 12.43±0.46(Predicted) |
| 形态 | 固体 |
| 颜色 | 灰白色至浅黄色 |
Ki: 12.2 nM (Neutrophil elastase)
Simulated extracorporeal circulation is established by recirculating fresh heparinized (3.75 U/mL) human blood for 120 minutes in a membrane oxygenator and a roller pump with and without 1.0 μM of Freselestat (ONO-6818). Neutrophil elastase levels are significantly lower in the Freselestat group. Freselestat significantly reduces interleukin 8 and C5b-9 production. Freselestat does not modulate changes of CD11b and L-selectin during recirculation.
Freselestat (ONO-6818; 10-100 mg/kg; oral administration; daily; for 8 weeks) treatment attenuates dose-dependently HNE-induced increases in lung myeloperoxidase activity, hemoglobin, and neutrophil count in bronchoalveolar lavage fluid. ONO-6818 inhibits acute lung injury induced by HNE by minimizing lung hemorrhage and accumulation of neutrophils in the lung.
| Animal Model: | Male Wistar rats (228 g) induced by human neutrophil elastase (HNE) |
| Dosage: | 10 mg/kg, 100 mg/kg |
| Administration: | Oral administration; daily; for 8 weeks |
| Result: | Attenuated dose-dependently HNE-induced increases in lung myeloperoxidase activity, hemoglobin, and neutrophil count in bronchoalveolar lavage fluid. |