产品描述: MBX-2982 is a selective, orally-available G protein-coupled receptor 119 (GPR119) agonist. |
靶点:
GPR119;GPR |
体内研究:
To examine whether the observations in GLUTag and the primary intestinal cells has physiological relevance, C57BL/6 mice are treated with the GPR119 agonist MBX-2982 at a dose of 10 mg/kg. Note that in order to examine a direct GPR119 effect, no DPP-IV inhibitor is co-administered in this experiment, but a DPP-IV inhibitor is used to preserve active GLP-1 in the blood samples. The plasma GLP-1 levels from the mice dosed with MBX-2982 are increased without a glucose load, indicating that GPR119-mediated GLP-1 secretion is not dependent on glucose |
参考文献:
1. Hothersall JD, et al. Sustained wash-resistant receptor activation responses of GPR119 agonists. Eur J Pharmacol. 2015 Sep 5;762:430-42. 2. Lan H, et al. Agonists at GPR119 mediate secretion of GLP-1 from mouse enteroendocrine cells through glucose-independent pathways. Br J Pharmacol. 2012 Apr;165(8):2799-807. 3. Yang JW, et al. GPR119: a promising target for nonalcoholic fatty liver disease. FASEB J. 2016 Jan;30(1):324-35. |
溶解性:
Soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.229 ml |
11.147 ml |
22.295 ml |
5 mM |
0.446 ml |
2.229 ml |
4.459 ml |
10 mM |
0.223 ml |
1.115 ml |
2.229 ml |
50 mM |
0.045 ml |
0.223 ml |
0.446 ml |
|
注意: |
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