| 产品描述: | TD-0212 TFA is an orally active dual pharmacology angiotensin II type 1 receptor (AT1) antagonist and neprilysin (NEP) inhibitor, with a pKi of 8.9 for AT1 and a pIC50 of 9.2 for NEP. |
| 体外研究: |
TD-0212 produces blood pressure reductions similar to omapatrilat and combinations of AT1 receptor antagonists and NEP inhibitors in models of renin-dependent and -independent hypertension[1]. |
| 体内研究: |
TD-0212 provides the enhanced activity of dual AT1/NEP inhibition with a potentially lower risk of angioedema relative to dual ACE/NEP inhibition. |
| 参考文献: |
1. McKinnell RM, et al. Discovery of TD-0212, an Orally Active Dual Pharmacology AT1 Antagonist and Neprilysin Inhibitor (ARNI). ACS Med Chem Lett. 2018 Dec 3;10(1):86-91. |
| 保存条件: |
-80°C 6个月; -20°C 1个月, 干燥 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.558 ml |
7.792 ml |
15.584 ml |
| 5 mM |
0.312 ml |
1.558 ml |
3.117 ml |
| 10 mM |
0.156 ml |
0.779 ml |
1.558 ml |
| 50 mM |
0.031 ml |
0.156 ml |
0.312 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。 |