CAS NO: | 1599477-75-4 |
包装 | 价格(元) |
5mg | 电议 |
10mg | 电议 |
50mg | 电议 |
Physical Appearance | A crystalline solid |
Storage | Store at -20°C |
M.Wt | 405.8 |
Cas No. | 1599477-75-4 |
Formula | C19H23ClF3NO3 |
Synonyms | GPR120 cpdA |
Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
Chemical Name | 3-[2-chloro-5-(trifluoromethoxy)phenyl]-3-azaspiro[5.5]undecane-9-acetic acid |
Canonical SMILES | OC(CC(CC1)CCC21CCN(C3=CC(OC(F)(F)F)=CC=C3Cl)CC2)=O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
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].
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.