Biological Activity
GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of −7.62.
In Vitro
GPR120-IN-1 is fully selective for Gpr120 (logEC50=−7.62) with negligible activity towards Gpr40. GPR120-IN-1 produces concentration dependent increases in IP3 production from both human and mouse Gpr120 expressing cells. GPR120-IN-1 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-IN-1 strongly and comparably inhibits LPS-induced phosphorylation of Tak1, Ikkβ, and Jnk and blocked IκB degradation [1].
In Vivo
GPR120-IN-1 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-IN-1 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[1].
References & source
Published experimental findings depend on the model and assay conditions. They do not guarantee equivalent performance in every application. For laboratory research use only.
