| 靶点: |
EC50: 60 nM (Glucokinase) |
| 体内研究: |
AZD1656 (0-9 mg/kg;灌胃;每天;持续 8 周;C57BL/6 小鼠) 处理显示血糖和葡萄糖波动降低以及胰岛素升高。AZD1656 增加了各种 ChREBP 靶基因 (包括碳水化合物反应元件结合蛋白 β 亚型 (ChREBP-β)、G6pc、Pklr、Acly、Acac 和 Gpd2) 的肝脏 mRNA 水平。 |
| 参考文献: |
1. Brian E Ford, et al. Chronic glucokinase activator treatment activates liver Carbohydrate response element binding protein and improves hepatocyte ATP homeostasis during substrate challenge. Diabetes Obes Metab. 2020 Jun 10. 2. Medicinal Chemistry, et al. Design and Development of the Glucokinase Activator AZD1656. Complete Accounts of Integrated Drug Discovery and Development: Recent Examples from the Pharmaceutical Industry Volume 1, 185-220.3. Terri Mitchard, et al. The novel use of a heterozygous knockout mouse for embryofetal development assessment of a glucokinase activator. Birth Defects Res B Dev Reprod Toxicol. 2014 Apr;101(2):152-61. |
| 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 |
2.09 ml |
10.449 ml |
20.899 ml |
| 5 mM |
0.418 ml |
2.09 ml |
4.18 ml |
| 10 mM |
0.209 ml |
1.045 ml |
2.09 ml |
| 50 mM |
0.042 ml |
0.209 ml |
0.418 ml |
|
| 注意: |
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