GPR120 Compound A

Modify Date: 2024-01-11 09:53:58

GPR120 Compound A Structure
GPR120 Compound A structure
Common Name GPR120 Compound A
CAS Number 1599477-75-4 Molecular Weight 405.83900
Density N/A Boiling Point N/A
Molecular Formula C19H23ClF3NO3 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of GPR120 Compound A


GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of −7.62.

 Names

Name 2-(3-(2-chloro-5-(trifluoromethoxy)phenyl)-3-azaspiro[5.5]undecan-9-yl)acetic acid
Synonym More Synonyms

 GPR120 Compound A 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

[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.

 Chemical & Physical Properties

Molecular Formula C19H23ClF3NO3
Molecular Weight 405.83900
Exact Mass 405.13200
PSA 49.77000
LogP 5.55510
Storage condition 2-8℃

 Synonyms

GPR120 Compound A
GPR120-IN-1