Cas No.: | 1599477-75-4 |
Chemical Name: | GPR120-IN-1 |
Synonyms: | GPR120-IN-1;GPR120 Compound A;GPR120 Agonist 3 |
SMILES: | O=C(O)CC(CC1)CCC21CCN(C3=CC(OC(F)(F)F)=CC=C3Cl)CC2 |
Formula: | C19H23ClF3NO3 |
M.Wt: | 405.839035272598 |
Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
Description: | GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of −7.62. |
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]. |
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]. |