Eprotirome-KB2115-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEEprotiromeCat. No.: HY-10473CAS No.: 355129-15-6Synonyms: KB2115分式: CHBrNO分量: 487.14作靶點(diǎn): Thyroid Hormone Receptor作通路: Others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 (256.60 mM; Need

2、ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.0528 mL 10.2640 mL 20.5280 mL5 mM 0.4106 mL 2.0528 mL 4.1056 mL10 mM 0.2053 mL 1.0264 mL 2.0528 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

3、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: 2.08 mg/mL (4.27 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 (4.27 mM); Clear solution3. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.27 m

4、M); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Eprotirome個(gè)肝臟選擇性甲狀腺激素受體激動(dòng)劑。IC50 & Target Thyroid hormone receptor 1體內(nèi)研究 Eprotirome is a liver-selective thyroid hormone receptor agonist. Histological analysis of livers from micetreated with Eprotirome reveals

5、 that Eprotirome elicits a near complete elimination of lipid filled vacuoles thatare characteristic of the livers from untreated control mice. Eprotirome treated mice also exhibit increasedfasting glucose, but Eprotirome does not increase fasting insulin levels. Glucose levels of mice treated withE

6、protirome continues to increase over time, leading to pronounced hyperglycemia by the end of the study.Temperature of mice treated with Eprotirome is decreased relative to untreated control mice 1.PROTOCOLAnimal Twelve-week old male ob/ob mice are used in this study. A catheter is implanted into the

7、 right internal jugularAdministration 1 vein before the hyperinsulinemic-euglycemic clamp. After recovery, mice are administered Eprotirome (0.3mg/kg) via intraperitoneal injection for 10 days. On the day of the clamp experiment, conscious, overnight-fasted mice receive a primed (10 Ci) and constant

8、 rate intravenous infusion (0.1 Ci /min) of 3-3H glucoseto measure basal glucose turnover. After 60 to 75 minutes of labeled glucose infusion, the hyperinsulinemic-euglycemic clamp is performed with continuous infusion of insulin (12 mU/kg/min) and variable infusion of25% glucose to maintain euglyce

9、mia (120 mg/dL). Blood samples are collected by tail bleeding(approximately every 10 min) to measure blood glucose concentrations 1.MCE has not independently confirmed the accuracy of these methods. They are for reference only.REFERENCES1. Martagn AJ, et al. The amelioration of hepatic steatosis by thyroid hormone receptor agonists is insufficient to restore insulin sensitivityin ob/ob mice. PLoS One. 2015 Apr 7;10(4):e0122987.McePdfHeightCaution: Product has not been fully validated fo