Sobetirome-GC-1-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemESobetiromeCat. No.: HY-14823CAS No.: 211110-63-3Synonyms: GC-1; QRX-431分式: CHO分量: 328.4作靶点: Thyroid Hormone Receptor作通路: Others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 : 9.85 mg/mL (29

2、.99 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 3.0451 mL 15.2253 mL 30.4507 mL5 mM 0.6090 mL 3.0451 mL 6.0901 mL10 mM 0.3045 mL 1.5225 mL 3.0451 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。BIOLOGICAL ACTIVITY物活性 Sobetirome种甲状腺激素受体 (TR) 激动剂，Sobetirome可选择性结合到TR-1，EC50 为 0

3、.16 M。IC50 & Target EC50: 0.16 M (TR-1), 0.58 M (TR-1) 1体内研究Sobetirome (GC-1) is a thyroid hormone receptor (TR)- and liver uptake-selective agonist. Sobetirome (481/3 Master of Small Molecules 您边的抑制剂师www.MedChemEnmol/kg) reduces high-density lipoprotein (HDL) cholesterol and very low-density lipopr

4、otein (VLDL)triglyceride levels in euthyroid Mice. Sobetirome reduces HDL cholesterol and triglyceride Levels inhypercholesterolemic mice. Sobetirome increases hepatic HDL receptors and stimulates bile acid synthesisin hypercholesterolemic mice 2. Treatment with 10 Sobetirome (GC-1) results in a gai

5、n of fat mass of only21% (1.7 g), and treatment with 20 Sobetirome (GC-1) induces a decrease in fat mass of 20% (1.3 g) 3.PROTOCOLAnimal Mice 2Administration 23 One hundred eighteen male C57BL/6 mice, 3 months old, are kept in standardized conditions with freeaccess to water and normal chow. 3,5,3-t

6、riiodo-L-thyronine (T3) or Sobetirome is administered i.p. in 20%DMSO or propylene glycol for 8 days, once daily at 9:00 a.m.; controls receive vehicle. In one experiment,nine groups of six mice are treated with vehicle, or 5.4, 24, 48, and 97 nmol/kg per day of T3 or Sobetirome.The lowest dose of T

7、3 induces euthyroidism in hypothyroid mice. In another experiment, one group of sevenmice is given no additional supplementation; three groups of seven mice receive 10% corn oil and 2%cholesterol (cholesterol diet); and three groups of seven mice receive 10% corn oil, 2% cholesterol, and 0.5%cholic

8、acid (cholic acid diet). For this experiment, mice are treated with vehicle or 97 nmol/kg per daySobetirome or T3. Food is withdrawn 5 h before kill. Blood is drawn by cardiac puncture under light isofluraneanesthesia. Animals are killed by cervical dislocation. Livers are immediately frozen in liqu

9、id nitrogen. Foranalysis of bile acid excretion, three groups of five chow-fed mice are treated with vehicle, 48 nmol/kg perday of Sobetirome, or T3 for 5 days. Feces are collected group-wise 24 h before treatment and in the last 24h of the experiment.Rats 3Female Wistar rats are randomly divided in

10、to five groups (n=8 per group): (i) control, treated with saline; (ii)10 T3, treated with 3 g T3/100 g body weight (BW) per day, which is equivalent to ten times thephysiological dose of T3; (iii) 20 T3, treated with double of the previous T3 dosage (6 g T3/100 g bodyweight (BW) per day); (iv) 10 So

11、betirome, treated with 1.5 g Sobetirome/100 g BW per day and (v) 20Sobetirome, treated with 3 g Sobetirome/100 g BW per day. The latter two groups are treated withSobetirome in equimolar doses of 10 T3 and 20 T3 respectively. The equimolar doses of Sobetirome arecalculated from the molecular mass of

12、 T3 (mol mass=651) and Sobetirome (mol mass=328.4). T3 isdissolved in 40 mM NaOH, and Sobetirome is dissolved in DMSO to a concentration of 1 mg/mL; either T3 orSobetirome are then diluted in saline and administered i.p. every day for 6 weeks. BW is measured thrice aweek. Body length (nose to base o

13、f the tail) is determined at the end of the experimental period.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 Am J Pathol. 2017 Nov;187(11):2473-2485. Gene Expr. 2016;17(1):19-34.See more customer validations on HYPERLINK / www.MedChemEREF

14、ERENCES2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE1. Gierach I, et al. Bacterial biosensors for screening isoform-selective ligands for human thyroid receptors -1 and -1. FEBS Open Bio.2012 Aug 15;2:247-53.2. Johansson L, et al. Selective thyroid receptor modulation by GC-1 reduces serum lipids and stimulates steps of reverse cholesteroltransport in euthyroid mice. Proc Natl Acad Sci U S A. 2005 Jul 19;102(29):10297-302.3. Villicev CM, et al. Thyroid hormone receptor beta-specific agonist GC-1 increases energy expenditure and prevents fat-massaccumulation in rats. J Endocrino