GPR120-IN-1 - GPR120 Agonist - 生命科學(xué)試劑 - 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作靶點(diǎn): GPR120作通路: GPCR/G Protein儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 50 mg/mL (123.20 mM)* means soluble, bu

2、t saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液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請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn)請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)

3、備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (6.16 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (6.16 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oil1/2 Master of Small Mol

4、ecules 您邊的抑制劑師www.MedChemESolubility: 2.5 mg/mL (6.16 mM); Clear solutionBIOLOGICAL ACTIVITY物活性 GPR120-IN-1是選擇性的Gpr120激動(dòng)劑，logEC50值為7.62。IC50 & Target logEC50: 7.62 1體外研究 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.體內(nèi)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.戶使本產(chǎn)品發(fā)表的科研獻(xiàn) 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