產(chǎn)品描述: | MK-8245 is a potent, liver-targeted stearoyl-CoA desaturase (SCD) inhibitor, with IC50s of 1 nM for human SCD1 and 3 nM for both rat SCD1 and mouse SCD1, with antidiabetic and antidyslipidemic efficacy |
靶點: |
IC50: 1 nM (human SCD1), 3 nM (rat SCD1), 3 nM (mouse SCD1);Dehydrogenase;Stearoyl-CoADesaturase(SCD) |
體內(nèi)研究: |
MK-8245 (10mg/kg; p.o.) exhibits a tissue distribution profile concentrated in the liver, with low exposure in tissues associated with potential adverse events in rats, dogs, and rhesus monkeys. MK-8245 improves glucose clearance in a dose-dependent manner in eDIO mice administrated before the glucose challenge |
參考文獻(xiàn): |
1. Oballa RM, et al. Development of a liver-targeted stearoyl-CoA desaturase (SCD) inhibitor (MK-8245) to establish a therapeutic window for the treatment of diabetes and dyslipidemia.J Med Chem. 2011 Jul 28;54(14):5082-96. Epub 2011 Jun 28. |
溶解性: |
Soluble in DMSO |
保存條件: |
-20℃ |
配置溶液濃度參考: |
|
1mg |
5mg |
10mg |
1 mM |
2.14 ml |
10.701 ml |
21.401 ml |
5 mM |
0.428 ml |
2.14 ml |
4.28 ml |
10 mM |
0.214 ml |
1.07 ml |
2.14 ml |
50 mM |
0.043 ml |
0.214 ml |
0.428 ml |
|
注意: |
部分產(chǎn)品我司僅能提供部分信息,我司不保證所提供信息的權(quán)威性,僅供客戶參考交流研究之用。 |