GPR120 Agonist 3

GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC₅₀ of 7.62. IC50 & Target: logEC50: 7.62^[1] In Vitro: 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 ^[1]. In Vivo: 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^[1].