| 靶点: |
IC50: 31 nM (BCAT1), 153 nM (BCAT2) |
| 体内研究: |
BAY-069 exhibits high metabolic stability after incubation with human liver microsomes (CLblood = 0.11 L/h/kg) and moderate metabolic stability after incubation with rat hepatocytes (CLblood = 1.8 L/h/kg); shows high permeability through Caco-2 cell monolayers with no hint of efflux. BAY-069 (0.3 mg/kg for i.v.; 0.6 mg/kg for p.o.; single dosage) exhibits a favorable pharmacokinetic profile after i.v. dosing with low blood clearance (CLblood), moderate volume of distribution at steady state (Vss), and intermediate terminal half-life (t1/2). |
| 参考文献: |
1. Günther J, et al. BAY-069, a Novel (Trifluoromethyl)pyrimidinedione-Based BCAT1/2 Inhibitor and Chemical Probe. J Med Chem. 2022 Oct 19. |
| 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 |
2.238 ml |
11.19 ml |
22.381 ml |
| 5 mM |
0.448 ml |
2.238 ml |
4.476 ml |
| 10 mM |
0.224 ml |
1.119 ml |
2.238 ml |
| 50 mM |
0.045 ml |
0.224 ml |
0.448 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。 |