| 靶点: |
Ki: 7.4 nM (Human adenosine A1 receptor) |
| 体内研究: |
Tonapofylline (BG 9928) (1 mg/kg;p.o.,每日两次,第 0-6 天) 能持续降低 NSC 119875 给药后血清肌酐和血尿素氮水平,促进体重恢复,并显著减弱 NSC 119875 (5.5 mg/kg) 诱导的肾脏病理评分。 |
| 参考文献: |
1. Kiesman WF, et al. Potent and orally bioavailable 8-bicyclo[2.2.2]octylxanthines as adenosine A1 receptor antagonists. J Med Chem. 2006 Nov 30;49(24):7119-31. 2. Ensor CR, et al. Tonapofylline: a selective adenosine-1 receptor antagonist for the treatment of heart failure. Expert Opin Pharmacother. 2010 Oct;11(14):2405-15. 3. Gill A, et al. Protective effect of tonapofylline (BG9928), an adenosine A1 receptor antagonist, against NSC 119875-induced acute kidney injury in rats. Am J Nephrol. 2009;30(6):521-6. |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.401 ml |
12.005 ml |
24.01 ml |
| 5 mM |
0.48 ml |
2.401 ml |
4.802 ml |
| 10 mM |
0.24 ml |
1.2 ml |
2.401 ml |
| 50 mM |
0.048 ml |
0.24 ml |
0.48 ml |
|
| 注意: |
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