| 靶点: |
IC50: 310 nM (CYP11B1), 2.1 nM (CYP11B2) |
| 体内研究: |
After oral administration in cyno monkeys, BI 689648 (5 mg/kg) exhibits a peak plasma concentration of ~500 nM. For BI 689648 (aldosterone EC50=2 nM), appreciable changes in 11-DOC are only noted at plasma concentrations >2000 nM or >1000-fold its aldosterone EC50 while FAD286 shows a window of ~100-fold. BI 689648 exhibits minimal impact on 11-DC and only at very high plasma concentrations (~10 μM). |
| 参考文献: |
1. Weldon SM, et al. Selectivity of BI 689648, a Novel, Highly Selective Aldosterone Synthase Inhibitor: Comparison with FAD286 and LCI699 in Nonhuman Primates. J Pharmacol Exp Ther. 2016 Oct;359(1):142-50. |
| 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 |
3.352 ml |
16.759 ml |
33.519 ml |
| 5 mM |
0.67 ml |
3.352 ml |
6.704 ml |
| 10 mM |
0.335 ml |
1.676 ml |
3.352 ml |
| 50 mM |
0.067 ml |
0.335 ml |
0.67 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |