GPR120-IN-1 - GPR120 Agonist - 生命科学试剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGPR120-IN-1Cat. No.: HY-101492CAS No.: 1599477-75-4分式: CHClFNO分量: 405.84作靶点: GPR120作通路: GPCR/G Protein储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO : 50 mg/mL (123.20 mM)* means soluble, bu

2、t saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4640 mL 12.3201 mL 24.6403 mL5 mM 0.4928 mL 2.4640 mL 4.9281 mL10 mM 0.2464 mL 1.2320 mL 2.4640 mL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，并请注意储备液的保存式和期限。体内实验请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄清的储备液，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄清的储

3、备液可以根据储存条件，适当保存；以下溶剂前的百分 指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.16 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.16 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oil1/2 Master of Small Mol

4、ecules 您边的抑制剂师www.MedChemESolubility: 2.5 mg/mL (6.16 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 GPR120-IN-1是选择性的Gpr120激动剂，logEC50值为7.62。IC50 & Target logEC50: 7.62 1体外研究 GPR120-IN-1 is fully selective for Gpr120 (logEC50=7.62) with negligible activity towards Gpr40. GPR120-IN-1 produces concentratio

5、n dependent increases in IP3 production from both human and mouse Gpr120expressing cells. GPR120-IN-1 leads to a concentration-dependent response to recruit -arrestin-2 in bothhuman and mouse Gpr120 expressing cells, with EC50s of 0.35 M. GPR120-IN-1 strongly and comparablyinhibits LPS-induced phosp

6、horylation of Tak1, Ikk, and Jnk and blocked IB degradation 1.体内研究 GPR120-IN-1 causes improved insulin sensitivity with increased glucose infusion rates, enhanced insulinstimulated-glucose disposal rate, along with a marked increase in the ability of insulin to suppress hepaticglucose production onl

7、y in WT mice. GPR120-IN-1 treatment has beneficial effects on hepatic lipidmetabolism, causing decreased hepatic steatosis, decreased liver triglycerides, and DAGs, along withreduced saturated free fatty acid conten 1.PROTOCOLAnimal Mice: Male C57Bl/6 WT or Gpr120 KO littermates are fed a normal cho

8、w (13.5% fat) or high-fat diet (60% fat)Administration 1 ad libitum for 15-20 weeks from 8 weeks of age. After 15 weeks on HFD, WT and Gpr120 KO mice areswitched to an isocaloric HFD supplemented with 3-FA concentrate or 30 mg/kg GPR120-IN-1 and fed for 5weeks. Mice receive fresh diet every 3rd day,

9、 and food consumption and body weight are monitored 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.户使本产品发表的科研献 Acta Physiol (Oxf). 2019 May;226(1):e13215.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Oh DY, et al. A Gpr120-selective agonist improves insulin resistance and chronic inflammation in obese mice. Nat Med. 2014Aug;20(8):942-7.McePdfHeightCaution: Product has not been fully validated for