Gly-β-MCA - FXR 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGly-MCACat. No.: HY-114392CAS No.: 66225-78-3分式: CHNO分量: 465.62作靶點(diǎn): FXR作通路: Metabolic Enzyme/Protease儲(chǔ)存式: Powder -20C 3 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 125 mg/mL (268.46 mM; Need ultrasonic)Mass Solvent

2、1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.1477 mL 10.7384 mL 21.4767 mL5 mM 0.4295 mL 2.1477 mL 4.2953 mL10 mM 0.2148 mL 1.0738 mL 2.1477 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)娜芙獍福渲魄罢?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)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

3、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: 2.08 mg/mL (4.47 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.47 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.47 mM); Clear solution1/2 M

4、aster of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Gly-MCA種膽汁酸， 有效的、穩(wěn)定的、腸特異性的以及具有服物活性的法尼酯X受體 (FXR) 抑制劑，可能會(huì)成為治療代謝障礙的候選藥物 1。IC50 & Target FXR 1.體外研究 Gly-MCA, a bile acid, is a potent, sable and intestine-selective and farnesoid X receptor (FXR) inhibitor 1.Gly-MCA (Gly-MCA, ) is resist

5、ant to hydrolysis by BSH 1.體內(nèi)研究 Gly-MCA (Gly-MCA, p.o. 10 and 50 mg/kg) prevents and treats diet-induced and genetic obesity, alongwith insulin resistance and hepatic steatosis without systemic, hepatic or intestinal toxicities in mice 1.Gly-MCA does not increase faecal LCN-2 levels, indicating that

6、 Gly-MCA does not induce intestinalinflammation 1.REFERENCES1. Jiang C, et al. Intestine-selective farnesoid X receptor inhibition improves obesity-related metabolic dysfunction. Nat Commun. 2015 Dec15;6:10166.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Tel: 400-82