GPR120 Compound A
Names
Biological Activity
[Description]:
GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of −7.62.
[Related Catalog]:
[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 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].
[Animal admin]
Mice: Male C57Bl/6 WT or Gpr120 KO littermates are fed a normal chow (13.5% fat) or high-fat diet (60% fat) ad libitum for 15-20 weeks from 8 weeks of age. After 15 weeks on HFD, WT and Gpr120 KO mice are switched to an isocaloric HFD supplemented with ω3-FA concentrate or 30 mg/kg GPR120-IN-1 and fed for 5 weeks. Mice receive fresh diet every 3rd day, and food consumption and body weight are monitored[1].
[References]
[Related Small Molecules]
Chemical & Physical Properties
[ Molecular Formula ]:
C19H23ClF3NO3
[ Molecular Weight ]:
405.83900
[ Exact Mass ]:
405.13200
[ PSA ]:
49.77000
[ LogP ]:
5.55510
[ Storage condition ]:
2-8℃