2. Vitamin D Related/Nuclear Receptor
  3. Thyroid Hormone Receptor
  4. Sobetirome

Sobetirome  (Synonyms: GC-1; QRX-431)

Cat. No.: HY-14823 Purity: 99.92%
COA Handling Instructions

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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.

For research use only. We do not sell to patients.

Sobetirome Chemical Structure

Sobetirome Chemical Structure

CAS No. : 211110-63-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 132 In-stock
Solution
10 mM * 1 mL in DMSO USD 132 In-stock
Solid
1 mg USD 48 In-stock
5 mg USD 120 In-stock
10 mg USD 180 In-stock
25 mg USD 432 In-stock
50 mg USD 732 In-stock
100 mg USD 1090 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 7 publication(s) in Google Scholar

Sobetirome Related Antibodies

Top Publications Citing Use of Products

    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: 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.

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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[1].

    IC50 & Target

    EC50: 0.16 μM (TRβ-1), 0.58 μM (TRα-1)[1]
    In Vivo

    Sobetirome (GC-1) is a thyroid hormone receptor β (TRβ)- and liver uptake-selective agonist. Sobetirome (48 nmol/kg) reduces high-density lipoprotein (HDL) cholesterol and very low-density lipoprotein (VLDL) triglyceride levels in euthyroid Mice. Sobetirome reduces HDL cholesterol and triglyceride Levels in hypercholesterolemic mice. Sobetirome increases hepatic HDL receptors and stimulates bile acid synthesis in hypercholesterolemic mice[2]. Treatment with 10× Sobetirome (GC-1) results in a gain of fat mass of only 21% (1.7 g), and treatment with 20× Sobetirome (GC-1) induces a decrease in fat mass of 20% (1.3 g)[3].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    Molecular Weight

    328.40

    Formula

    C20H24O4
    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    O=C(O)COC1=CC(C)=C(CC2=CC=C(O)C(C(C)C)=C2)C(C)=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 3.0451 mL 15.2253 mL 30.4507 mL
    5 mM 0.6090 mL 3.0451 mL 6.0901 mL
    View the 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.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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.
    Purity & Documentation

    Purity: 99.92%

    COA (244 KB) LCMS (263 KB)

    Handling Instructions (2659 KB)
    References
    Animal Administration
    [2][3]

    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.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    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
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    Sobetirome Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Sobetirome211110-63-3GC-1 QRX-431GC1GC 1QRX431QRX 431QRX-431Thyroid Hormone ReceptorTHRInhibitorinhibitorinhibit

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