| 靶点: |
IC50: 53 nM (rat liver ACC1) and 61 nM (rat skeletal muscle ACC2) |
| 体内研究: |
CP-640186 (口服灌胃;4.6-21 mg/kg;一次) 显示出急性疗效。 CP-640186 (静脉注射和口服灌胃;静脉剂量,5 mg/ kg;口服剂量,10 mg/kg;一次) 在相同剂量下,大鼠的药物暴露低于 ob/ob 小鼠。 CP-640186 (口服强饲法;100 mg/kg;一次) 处理显示在高暴露水平下从碳水化合物利用完全转变为脂肪酸利用作为能量来源。 |
| 参考文献: |
1. Harwood HJ Jr, et al. Isozyme-nonselective N-substituted bipiperidylcarboxamide acetyl-CoA carboxylase inhibitors reduce tissue malonyl-CoA concentrations, inhibit fatty acid synthesis, and increase fatty acid oxidation in cultured cells and in experimental animals. J Biol Chem. 2003 Sep 26;278(39):37099-111. 2. Yamashita T, et al. Design, synthesis, and structure-activity relationships of spirolactones bearing 2-ureidobenzothiophene as acetyl-CoA carboxylases inhibitors. Bioorg Med Chem Lett. 2011 Nov 1;21(21):6314-8. 3. Daniel Hess, et al. Inhibition of stearoylCoA desaturase activity blocks cell cycle progression and induces programmed cell death in lung cancer cells. PLoS One. 2010 Jun 30;5(6):e11394. |
| 保存条件: |
-80℃,干燥(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.915 ml |
9.577 ml |
19.154 ml |
| 5 mM |
0.383 ml |
1.915 ml |
3.831 ml |
| 10 mM |
0.192 ml |
0.958 ml |
1.915 ml |
| 50 mM |
0.038 ml |
0.192 ml |
0.383 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。 |