| Identification | Back Directory | [Name]
GPR120 Compound A | [CAS]
1599477-75-4 | [Synonyms]
MDK 77754
MDK-77754
GPR120 CPDA
GPR120-IN-1
GPR120 Compound A
GPR120 inhibitor 1
GPR120 COMPOUND A HCl
GPR120 CPDA;GPR120-IN-1;MDK-77754;MDK 77754
3-[2-Chloro-5-(trifluoromethoxy)phenyl]-3-azaspiro[5.5]undecane-9-acetic acid
3-Azaspiro[5.5]undecane-9-acetic acid, 3-[2-chloro-5-(trifluoromethoxy)phenyl]-
2-(3-(2-chloro-5-(trifluoromethoxy)phenyl)-3-azaspiro[5.5]undecan-9-yl)acetic acid | [Molecular Formula]
C19H23ClF3NO3 | [MOL File]
1599477-75-4.mol | [Molecular Weight]
405.84 |
| Chemical Properties | Back Directory | [Boiling point ]
506.0±50.0 °C(Predicted) | [density ]
1.35±0.1 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | [form ]
crystalline solid | [pka]
4.68±0.10(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
GPR120 Agonist 3 is a selective Gpr120 agonist with a logEC50 of 7.62. | [Biological Activity]
gpr120 compound a is an orally active and high-affinity agonist of gpr120 [1].g-protein coupled receptor 120 (gpr120, free fatty acid receptor 4/ffar4) is a g protein-coupled receptor which has been expressed in intestine, adipocytes, and pro-inflammatory macrophages that is activated by long chain free fatty acids. gpr120 has been involved in mediating the anti-inflammatory and insulin-sensitizing effects of omega 3 fatty acids. deficiency of gpr120 is responsible for reduced fat metabolism, produce anti-inflammatory effects and to acutely potentiate insulin secretion [2].gpr120 compound a activated gpr120 with the ec50 value of ~0.35 μm. gpr120 compound a demonstrated potent selectivity over another lipid-sensing g-protein, gpr40 (ffar1). in a high-fat diet fed obese mice, gpr120 compound a (30 mg/kg) exerted anti-inflammatory effects on macrophages in vitro and improved glucose tolerance, decreased hyperinsulinemia, increased insulin sensitivity, and decreased hepatic steatosis [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]. | [storage]
Store at -20°C | [References]
[1] walenta e, akiyama t e, lagakos w s, et al. a gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice[j]. nature medicine, 2014, 20(8): 942-947.
[2] ichimura a, hirasawa a, poulain-godefroy o, et al. dysfunction of lipid sensor gpr120 leads to obesity in both mouse and human[j]. nature, 2012, 483(7389): 350-354. |
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