| 靶点: |
Ki: 12.2 nM (Neutrophil elastase) |
| 体内研究: |
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. |
| 参考文献: |
1. Am J Respir Crit Care Med. 2002 Aug 15;166(4):496-500. 2. K Ohmoto, et al. Design and synthesis of new orally active inhibitors of human neutrophil elastase. Bioorg Med Chem. 2001 May;9(5):1307-23. 3. Yasushi Hirota, et al. Effects of the neutrophil elastase inhibitor (ONO-6818) on acetic acid induced colitis in Syrian hamsters. J Vet Med Sci. 2004 Oct;66(10):1223-8. 4. Yukihiro Yoshimura, et al. ONO-6818, a novel, potent neutrophil elastase inhibitor, reduces inflammatory mediators during simulated extracorporeal circulation. Ann Thorac Surg. 2003 Oct;76(4):1234-9. |
| 保存条件: |
2-8℃ |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.21 ml |
11.049 ml |
22.099 ml |
| 5 mM |
0.442 ml |
2.21 ml |
4.42 ml |
| 10 mM |
0.221 ml |
1.105 ml |
2.21 ml |
| 50 mM |
0.044 ml |
0.221 ml |
0.442 ml |
|
| 注意: |
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