| 产品描述： | TUG-469 is a selective free fatty acid receptor 1 (FFA1/GPR40) agonist with an EC50 value of 19 nM. TUG-469 is >200-fold selective for FFA1 over FFA4. TUG-469 significantly improves glucose tolerance in pre-diabetic mice. TUG-469 can be used for the research of diabetes |
| 靶点： |
Free Fatty Acid Receptor |
| 体外研究： |
TUG-469 (0-10 μM) shows efficacy to hFFA1 with a pEC50 value of 7.73. TUG-469 (10 μM) increases the insulin secretion under 10 mM glucose stimulation. TUG-469 (0-100 μM) is >200-fold selective for FFA1 over FFA4 with EC50 values of 19 nM and 4.4 μM for FFA1 and FFA4, respectively. TUG-469 (5 μM; 30 min) significantly increases insulin secretion of INS-1 cells with the presence of high glucose concentration (16.7 mM) |
| 体内研究： |
TUG-469 (5 mg/kg; i.p.; 60 and 90 min after glucose administration) affects blood glucose level. Animal Model: Male NZO mice with glucose administration Dosage: 5 mg/kg Administration: Intraperitoneal injection; 5 mg/kg; 60 and 90 min after glucose administration Result: Reduced the blood glucose level. |
| 参考文献： |
1. Christiansen E, et al. Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469. ACS Med Chem Lett. 2010 Jul 2;1(7):345-9. 2. Urban C, et al. In vitro and mouse in vivo characterization of the potent free fatty acid 1 receptor agonist TUG-469. Naunyn Schmiedebergs Arch Pharmacol. 2013 Dec;386(12):1021-30. |
| 溶解性： |
Soluble in DMSO |
| 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 |
2.895 ml |
14.474 ml |
28.948 ml |
| 5 mM |
0.579 ml |
2.895 ml |
5.79 ml |
| 10 mM |
0.289 ml |
1.447 ml |
2.895 ml |
| 50 mM |
0.058 ml |
0.289 ml |
0.579 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