| 靶点： |
pEC50: 7.54 (FFA1/GPR40) |
| 体内研究： |
Single oral administration of GPR40 agonist 4 (compound 20) robustly reduces the plasma glucose excursion and enhances insulin secretion during an oral glucose tolerance test (OGTT) in a dose-dependent manner from 1 to 10 mg/kg when GPR40 agonist 4 is dosed 60 min prior to the oral glucose challenge. The area under the curve of blood glucose (AUC0-120min) and blood insulin (AUC0-120min) reveal that the minimum effective dose of GPR40 agonist 4 is 3 mg/kg. The hyperglycemia state is also markedly improved in GPR40 agonist 4 (20 mg/kg) treated group. |
| 参考文献： |
1. Li Z, et al. Discovery of phenylsulfonyl acetic acid derivatives with improved efficacy and safety as potent free fatty acid receptor 1 agonists for the treatment of type 2 diabetes. Eur J Med Chem. 2017 Sep 29;138:458-479. |
| 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 |
2.399 ml |
11.994 ml |
23.988 ml |
| 5 mM |
0.48 ml |
2.399 ml |
4.798 ml |
| 10 mM |
0.24 ml |
1.199 ml |
2.399 ml |
| 50 mM |
0.048 ml |
0.24 ml |
0.48 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京