GPR120 Agonist 3 是一种有效的、选择性的GPR120激动剂,logEC50为 ?7.62。
半岛bd体育手机客户端
描述
GPR120-IN-1 is a selective agonist of Gpr120 ( logEC50: -7.62).
体外活性
GPR120-IN-1 causes a concentration-dependent response to recruiting β-arrestin-2 in both human and mouse Gpr120 expressing cells(EC50s: ~0.35 μM). GPR120-IN-1 produces concentration-dependent increases in IP3 production from both human and mouse Gpr120 expressing cells. GPR120-IN-1 strongly and comparably inhibits LPS-induced phosphorylation of Ikkβ, Tak1, and Jnk and blocked IκB degradation.
体内活性
GPR120-IN-1 treatment has beneficial effects on hepatic lipid metabolism. It causes decreased liver triglycerides, decreased hepatic steatosis, and DAGs, as well as decreased saturated free fatty acid content. GPR120-IN-1 causes improved insulin sensitivity with increased glucose infusion rates. It also enhanced the insulin stimulated-glucose disposal rate. Only in WT mice, along with a marked increase in the ability of insulin to suppress hepatic glucose production.
Cas No.
1599477-75-4
分子式
C19H23ClF3NO3
分子量
405.84
别名
GPR120-IN-1
储存和溶解度
H2O:< 0.1 mg/mL (insoluble),Need ultrasonic and warming and heat to 60°C
DMSO:50 mg/mL (123.20 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years