GPR120-IN-1

1599477-75-4

C19H23ClF3NO3

DMSO : >= 50 mg/mL (123.20 mM)

GPCR/G Protein

GPR120-IN-1 is a selective Gpr120 agonist with a logEC₅₀ of ?7.62. IC50 & Target: logEC50: ?7.62^[1] 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 beta-arrestin-2 in both human and mouse Gpr120 expressing cells, with EC₅₀s of ca.0.35 uM. GPR120-IN-1 strongly and comparably inhibits LPS-induced phosphorylation of Tak1, Ikkbeta, and Jnk and blocked IkappaB 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].