GPR120-IN-1_DataSheet_MedChemExpress

Inhibitors, Agonists, Screening Libraries

https://www.wendangku.net/doc/1310212555.html, Data Sheet

BIOLOGICAL ACTIVITY:

GPR120–IN–1 is a selective Gpr120 agonist with a logEC 50 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 IP 3 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 EC 50s of ~0.35μM. 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].

PROTOCOL (Extracted from published papers and Only for reference)

Animal Administration:[1]Mouse: 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:

[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.

Product Name:

GPR120–IN–1Cat. No.:

HY-101492CAS No.:

1599477-75-4Molecular Formula:

C 19H 23ClF 3NO 3Molecular Weight:

405.84Target:

GPR120Pathway:

GPCR/G Protein Solubility:

10 mM in DMSO

Caution: Product has not been fully validated for medical applications. For research use only.

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