产品描述: GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of −7.62. |
靶点:
logEC50: −7.62;GPR |
体外研究:
GPR120 Agonist 3 is fully selective for Gpr120 (logEC50=−7.62) with negligible activity towards Gpr40. GPR120 Agonist 3 produces concentration dependent increases in IP3 production from both human and mouse Gpr120 expressing cells. GPR120 Agonist 3 leads to a concentration-dependent response to recruit β-arrestin-2 in both human and mouse Gpr120 expressing cells, with EC50s of ~0.35 μM. GPR120 Agonist 3 strongly and comparably inhibits LPS-induced phosphorylation of Tak1, Ikkβ, and Jnk and blocked IκB degradation |
体内研究:
GPR120 Agonist 3 causes improved insulin sensitivity with increased glucose infusion rates, enhanced insulin stimulated-glucose disposal rate, along with a marked increase in the ability of insulin to suppress hepatic glucose production only in WT mice. GPR120 Agonist 3 treatment has beneficial effects on hepatic lipid metabolism, causing decreased hepatic steatosis, decreased liver triglycerides, and DAGs, along with reduced saturated free fatty acid conten |
参考文献:
1. Oh DY, et al. A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice. Nat Med. 2014 Aug;20(8):942-7. |
溶解性:
soluble in DMSO |
保存条件:
-20℃ |
配置溶液浓度参考:
|
1mg |
5mg |
10mg |
1 mM |
2.464 ml |
12.32 ml |
24.64 ml |
5 mM |
0.493 ml |
2.464 ml |
4.928 ml |
10 mM |
0.246 ml |
1.232 ml |
2.464 ml |
50 mM |
0.049 ml |
0.246 ml |
0.493 ml |
|
注意: |
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