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  3. Sobetirome

Sobetirome (Synonyms: GC-1; QRX-431)

Cat. No.: HY-14823 Purity: 99.79%
Handling Instructions

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

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 132 In-stock
Estimated Time of Arrival: December 31
5 mg USD 120 In-stock
Estimated Time of Arrival: December 31
10 mg USD 180 In-stock
Estimated Time of Arrival: December 31
50 mg USD 732 In-stock
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Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Sobetirome purchased from MCE. Usage Cited in: Gene Expr. 2016;17(1):19-34.

    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.

    Sobetirome purchased from MCE. Usage Cited in: Am J Pathol. 2017 Nov;187(11):2473-2485.

    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)
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    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].

    Clinical Trial
    Molecular Weight

    328.40

    Formula

    C₂₀H₂₄O₄

    CAS No.

    211110-63-3

    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 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    Methanol : 125 mg/mL (380.63 mM; Need ultrasonic)

    DMSO : 100 mg/mL (304.51 mM; Need ultrasonic)

    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
    10 mM 0.3045 mL 1.5225 mL 3.0451 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 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

    • 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

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (7.61 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    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

    Purity: 99.79%

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    Keywords:

    SobetiromeGC-1 QRX-431GC1GC 1QRX431QRX 431QRX-431Thyroid Hormone ReceptorTHRInhibitorinhibitorinhibit

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    Product Name:
    Sobetirome
    Cat. No.:
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