| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 50mg | 电议 |
| 生物活性 | Freselestat quarterhydrate (ONO-6818 quarterhydrate) is a potent and orally activeneutrophilelastaseinhibitor with aKiof 12.2 nM. Freselestat quarterhydrate is >100-fold less-active against other proteases such as trypsin, protein-ase 3, pancreaticelastase, plasmin,thrombin, collagenase,cathepsinG, and murine macrophageelastase. Freselestat quarterhydrate has a potent anti-inflammatory activity[1][2][3][4]. | |||||||||
| IC50& Target | Ki: 12.2 nM (Neutrophil elastase)[3] | |||||||||
| 体外研究 (In Vitro) | 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[3]. | |||||||||
| 体内研究 (In Vivo) | 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[1].
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| 分子量 | 457.03 | |||||||||
| 性状 | Solid | |||||||||
| Formula | C23H28N6O4.1/4H2O | |||||||||
| 运输条件 | Room temperature in continental US; may vary elsewhere. | |||||||||
| 储存方式 |
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