Sobetirome
Based on 7 publication(s) in Google Scholar
Sobetirome (GC-1) is a thyroid hormone receptor β (TRβ)-specific agonist which bind selectively to TRβ-1 with an EC50 of 0.16 μM.
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- Pureté: 99.87%
- CAS No.: 211110-63-3
- Formule: C20H24O4
- Masse moléculaire:328.40
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Stockage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Protocole
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Publications Citing Use of MedChemExpress (MCE) Sobetirome
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Customer Validation & Images
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In Vivo Efficacy Study
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Histological Imaging/Staining
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WB
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In Vivo Efficacy Study
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In Vivo Efficacy Study
Activité biologique
EC50: 0.16 μM (TRβ-1), 0.58 μM (TRα-1)[1]
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 211110-63-3
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Appearance Solid
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Masse moléculaire 328.40
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Formule C20H24O4
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Color White to yellow
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SMILES
O=C(O)COC1=CC(C)=C(CC2=CC=C(O)C(C(C)C)=C2)C(C)=C1
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Synonyms
GC-1; QRX-431
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (7)
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Journal Impact Factor
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Most Recent
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Am J Pathol
The Thyromimetic Sobetirome (GC-1) Alters Bile Acid Metabolism in a Mouse Model of Hepatic Cholestasis. [Abstract]2020 May;190(5):1006-1017. PMID: 32205094
Sobetirome purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2020 May;190(5):1006-1017. [Abstract]
Biliary injury improves in ATP binding cassette subfamily B member 4 (Abcb4−/−; Mdr2−/−) knockout (KO) mice at 2 and 4 weeks after Sobetirome (GC-1), at the expense of hepatic injury. Blood serum levels of alkaline phosphatase (ALP) show decreased biliary injury, whereas alanine aminotransferase (ALT) and aspartate aminotransferase (AST) indicate increased hepatic injury, in KO mice on short-term GC-1 diet compared with KO mice.
Sobetirome purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2020 May;190(5):1006-1017. [Abstract]
Biliary injury improves in ATP binding cassette subfamily B member 4 (Abcb4−/−; Mdr2−/−) knockout (KO) mice at 2 and 4 weeks after Sobetirome (GC-1), at the expense of hepatic injury. Representative hematoxylin and eosin images show equivalent parenchymal injury in KO mice on GC-1 diet for 2 and 4 weeks compared with KO mice on normal diet.
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Am J Pathol
Thyroid Hormone Receptor-β Agonist GC-1 Inhibits Met-β-Catenin-Driven Hepatocellular Cancer. [Abstract]2017 Nov;187(11):2473-2485. PMID: 28807594
Sobetirome purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2017 Nov;187(11):2473-2485. [Abstract]
GC-1 treatment of hMet-mutant-β-catenin mice for 21-days leads to marked inhibition of Met signaling. A. A profound decrease in p-Met (Y1234/Y1235) is observed by WB analysis using whole liver lysates from GC-1 treated mice versus basal diet controls. A marginal but variable decrease in total Met was also evident in this group. GAPDH shows comparable loading. B. Another representative WB shows lack of p-Met (Y1234/1235) along with a dramatic decrease in downstream p-ERK1 (T202) and p-ERK2 (Y204)
Sobetirome purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2017 Nov;187(11):2473-2485. [Abstract]
RT-PCR using RNA isolated from livers shows around 40-fold increase in gene expression of deiodinase (DIOI) after 21 days of the Sobetirome (GC-1) diet as compared to the basal diet.
Sobetirome purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2017 Nov;187(11):2473-2485. [Abstract]
An almost significant (P = 0.0506) difference in liver weight/body weight (LW/BW × 100) is observed after 21 days of the Sobetirome (GC-1) diet as compared to the basal diet, suggesting a decrease in tumor burden. Individual animals in each group are indicated by a closed circle or closed square.
Sobetirome purchased from MedChemExpress. Usage Cited in: Am J Pathol. 2017 Nov;187(11):2473-2485. [Abstract]
Representative hematoxylin and eosin (H&E)-stained sections show relatively fewer and smaller microscopic hepatic tumor nodules in Sobetirome (GC-1)–treated group at 21 days.
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Int Immunol
The thyroid hormone receptor beta (TR-β) signaling controls pathogenic Th17 cells in autoimmune disease. [Abstract]2025 Dec 24;37(12):789-803. PMID: 40873150 -
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Gene Expr
Thyroid Hormone Receptor β Agonist Induces β-Catenin-Dependent Hepatocyte Proliferation in Mice: Implications in Hepatic Regeneration. [Abstract]2016;17(1):19-34. PMID: 27226410
Sobetirome purchased from MedChemExpress. Usage Cited in: Gene Expr. 2016;17(1):19-34. [Abstract]
Western blot of whole-liver lysates shows increased cyclin D1 and pSer675-β-catenin in GC-1-treated mice compared with DMSO control. Western blot analysis using whole-cell lysates from the livers from the two groups shows increased pSer675-β-catenin and cyclin D1 levels in the GC-1-treated group, while total β-catenin levels do not show much difference.
Solvant et solubilité
DMSO : 100 mg/mL (304.51 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (7.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (7.61 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocole
Mice[2]
One hundred eighteen male C57BL/6 mice, 3 months old, are kept in standardized conditions with free access to water and normal chow. 3,5,3′-triiodo-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 T3 induces euthyroidism in hypothyroid mice. In another experiment, one group of seven mice 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 acid (cholic acid diet). For this experiment, mice are treated with vehicle or 97 nmol/kg per day Sobetirome or T3. Food is withdrawn 5 h before kill. Blood is drawn by cardiac puncture under light isoflurane anesthesia. Animals are killed by cervical dislocation. Livers are immediately frozen in liquid nitrogen. For analysis of bile acid excretion, three groups of five chow-fed mice are treated with vehicle, 48 nmol/kg per day of Sobetirome, or T3 for 5 days. Feces are collected group-wise 24 h before treatment and in the last 24 h of the experiment.
Rats[3]
Female Wistar rats are randomly divided into five groups (n=8 per group): (i) control, treated with saline; (ii) 10× T3, treated with 3 μg T3/100 g body weight (BW) per day, which is equivalent to ten times the physiological dose of T3; (iii) 20× T3, treated with double of the previous T3 dosage (6 μg T3/100 g body weight (BW) per day); (iv) 10× Sobetirome, treated with 1.5 μg Sobetirome/100 g BW per day and (v) 20× Sobetirome, treated with 3 μg Sobetirome/100 g BW per day. The latter two groups are treated with Sobetirome in equimolar doses of 10× T3 and 20× T3 respectively. The equimolar doses of Sobetirome are calculated from the molecular mass of T3 (mol mass=651) and Sobetirome (mol mass=328.4). T3 is dissolved in 40 mM NaOH, and Sobetirome is dissolved in DMSO to a concentration of 1 mg/mL; either T3 or Sobetirome are then diluted in saline and administered i.p. every day for 6 weeks. BW is measured thrice a week. Body length (nose to base of the tail) is determined at the end of the experimental period.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (396 KB)
- English - EN (396 KB)
- Français - FR (396 KB)
- Deutsch - DE (396 KB)
- Norwegian - NO (396 KB)
- Español - ES (396 KB)
- Swedish - SV (396 KB)
- Italian - IT (396 KB)
- Korean - KR (396 KB)
- Portuguese - PT (396 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Gierach I, et al. Bacterial biosensors for screening isoform-selective ligands for human thyroid receptors α-1 and β-1. FEBS Open Bio. 2012 Aug 15;2:247-53. [Content Brief]
[2]. Johansson L, et al. Selective thyroid receptor modulation by GC-1 reduces serum lipids and stimulates steps of reverse cholesterol transport in euthyroid mice. Proc Natl Acad Sci U S A. 2005 Jul 19;102(29):10297-302. [Content Brief]
[3]. Villicev CM, et al. Thyroid hormone receptor beta-specific agonist GC-1 increases energy expenditure and prevents fat-mass accumulation in rats. J Endocrinol. 2007 Apr;193(1):21-9. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 3.0451 mL | 15.2253 mL | 30.4507 mL | 76.1267 mL |
| 5 mM | 0.6090 mL | 3.0451 mL | 6.0901 mL | 15.2253 mL | |
| 10 mM | 0.3045 mL | 1.5225 mL | 3.0451 mL | 7.6127 mL | |
| 15 mM | 0.2030 mL | 1.0150 mL | 2.0300 mL | 5.0751 mL | |
| 20 mM | 0.1523 mL | 0.7613 mL | 1.5225 mL | 3.8063 mL | |
| 25 mM | 0.1218 mL | 0.6090 mL | 1.2180 mL | 3.0451 mL | |
| 30 mM | 0.1015 mL | 0.5075 mL | 1.0150 mL | 2.5376 mL | |
| 40 mM | 0.0761 mL | 0.3806 mL | 0.7613 mL | 1.9032 mL | |
| 50 mM | 0.0609 mL | 0.3045 mL | 0.6090 mL | 1.5225 mL | |
| 60 mM | 0.0508 mL | 0.2538 mL | 0.5075 mL | 1.2688 mL | |
| 80 mM | 0.0381 mL | 0.1903 mL | 0.3806 mL | 0.9516 mL | |
| 100 mM | 0.0305 mL | 0.1523 mL | 0.3045 mL | 0.7613 mL |
Sobetirome Related Classifications
HY-14823 Related Classifications
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