| Bioactivity | GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of −7.62. | ||||||||||||
| Target | logEC50: −7.62 | ||||||||||||
| Invitro | 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]. | ||||||||||||
| Name | GPR120 Agonist 3 | ||||||||||||
| CAS | 1599477-75-4 | ||||||||||||
| Formula | C19H23ClF3NO3 | ||||||||||||
| Molar Mass | 405.84 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| Reference | [1]. Oh DY, et al. A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice. Nat Med. 2014 Aug;20(8):942-7. |