GPR120 Compound A
(Synonyms: GPR120 cpdA) 目录号 : GC14300
A selective GPR120/FFAR4 agonist
Cas No.:1599477-75-4
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
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.
Animal experiment: | 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. | |
| Cas No. | 1599477-75-4 | SDF | |
| 别名 | GPR120 cpdA | ||
| 化学名 | 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 | ||
| 分子式 | C19H23ClF3NO3 | 分子量 | 405.8 |
| 溶解度 | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.4643 mL | 12.3213 mL | 24.6427 mL |
| 5 mM | 0.4929 mL | 2.4643 mL | 4.9285 mL |
| 10 mM | 0.2464 mL | 1.2321 mL | 2.4643 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet