| 产品描述: | BAY-9835, a chemical probe, is an orally active ADAMTS7 and ADAMTS12 antagonist with IC50s of 6 nM and 30 nM, respectively. BAY-9835 exhibits inhibitory potencies vs mouse (mIC50 = 8 nM) and rat (rIC50 = 27 nM) ADAMTS7 enzymes. BAY-9835 is very selective against a range of off-targets and metalloproteases. BAY-9835 can be used for the study of atherogenesis. |
| 体内研究: |
BAY-9835 (Compound 32) 在与人微粒体孵育时表现出较高代谢稳定性 (Clbl = 10−4 L/h/kg),在人血浆中搅拌 24 小时未观察到降解。 BAY-9835 未检测到对 CYP1A2、2C8、2C9、2D6 和 3A4 酶的抑制 (< 20 μM),和对心脏离子通道 (hERG、hNav1.5、hCav1.2) 的抑制 (< 10 μM)。 |
| 参考文献: |
1. Daniel Meibom, et al. BAY-9835: Discovery of the First Orally Bioavailable ADAMTS7 Inhibitor. J Med Chem. 2024 Feb 22;67(4):2907-2940. |
| 保存条件: |
-80°C 12个月; -20°C 6个月,干燥, 避光 |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
2.027 ml |
10.134 ml |
20.268 ml |
| 5 mM |
0.405 ml |
2.027 ml |
4.054 ml |
| 10 mM |
0.203 ml |
1.013 ml |
2.027 ml |
| 50 mM |
0.041 ml |
0.203 ml |
0.405 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。 |