1599477-75-4
1599477-75-4 structure
- Name: GPR120 Compound A
- Chemical Name: 2-(3-(2-chloro-5-(trifluoromethoxy)phenyl)-3-azaspiro[5.5]undecan-9-yl)acetic acid
- CAS Number: 1599477-75-4
- Molecular Formula: C19H23ClF3NO3
- Molecular Weight: 405.83900
- Catalog: Signaling Pathways GPCR/G Protein GPR120
- Create Date: 2017-02-16 04:38:01
- Modify Date: 2024-01-11 09:53:58
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GPR120-IN-1 is a selective Gpr120 agonist with a logEC50 of −7.62.
| Name | 2-(3-(2-chloro-5-(trifluoromethoxy)phenyl)-3-azaspiro[5.5]undecan-9-yl)acetic acid |
|---|---|
| Synonyms |
GPR120 Compound A
GPR120-IN-1 |
| 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 |
| Molecular Formula | C19H23ClF3NO3 |
|---|---|
| Molecular Weight | 405.83900 |
| Exact Mass | 405.13200 |
| PSA | 49.77000 |
| LogP | 5.55510 |
| Storage condition | 2-8℃ |