GPR120 Agonist 3

• CAT Number: I013666
• CAS Number: 1599477-75-4
• Molecular Formula: C19H23ClF3NO3
• Molecular Weight: 405.84
• Purity: ≥95%
• Synonyms: 2-[3-[2-chloro-5-(trifluoromethoxy)phenyl]-3-azaspiro[5.5]undecan-9-yl]acetic acid
• InChI: InChI=1S/C19H23ClF3NO3/c20-15-2-1-14(27-19(21,22)23)12-16(15)24-9-7-18(8-10-24)5-3-13(4-6-18)11-17(25)26/h1-2,12-13H,3-11H2,(H,25,26)
• InChIKey: WUJVPELCYCESAP-UHFFFAOYSA-N
• SMILES: C1CC2(CCC1CC(=O)O)CCN(CC2)C3=C(C=CC(=C3)OC(F)(F)F)Cl

GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of −7.62.
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].
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].

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.
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