1. Vitamin D Related/Nuclear Receptor
  2. Thyroid Hormone Receptor
  3. Resmetirom

Resmetirom  (Synonyms: MGL-3196; VIA-3196)

Cat. No.: HY-12216 Purity: 99.93%
Handling Instructions Technical Support

Resmetirom (MGL-3196) is a highly selective and orally active thyroid hormone receptor β (THR-β) agonist with an EC50 value of 0.21 μM. Resmetirom can be used for the study of noncirrhotic nonalcoholic steatohepatitis.

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

CAS No. : 920509-32-6

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Customer Review

Based on 22 publication(s) in Google Scholar

Other Forms of Resmetirom:

Top Publications Citing Use of Products

    Resmetirom purchased from MedChemExpress. Usage Cited in: Nat Metab. 2024 Dec;6(12):2281-2299.  [Abstract]

    The experimental schedule showing the treatment of female 8-week-old C57BL/6J mice with Resmetirom (RES) (0.033 mg /mL or vehicle control per gavage). RES was prepared in 10% DMSO, 40% PEG300, 5% Tween 80 and 45% drinking water (v/v), at a final concentration of 0.033 mg /mL.

    Resmetirom purchased from MedChemExpress. Usage Cited in: Nat Metab. 2024 Dec;6(12):2281-2299.  [Abstract]

    The experimental schedule showing the treatment of female 8-week-old C57BL/6J mice with Resmetirom (RES) (0.033 mg /mL or vehicle control per gavage). RES was prepared in 10% DMSO, 40% PEG300, 5% Tween 80 and 45% drinking water (v/v), at a final concentration of 0.033 mg /mL.

    Resmetirom purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 Apr 15;6(4):102047.  [Abstract]

    C57BL/6J wild-type mice were fed FPC diet for 27 weeks. Drugs were administered from 19 to 27 weeks. 8 mg/kg of APB-R3 (SAFA-hIL-18BP) was intraperitoneally administered three times a week as indicated. 5 mg/kg of THRβ agonist (MGL-3196; Resmetirom) was daily orally gavaged as compared group. Plasma ALT and AST levels were measured at the end of experiments.

    Resmetirom purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 Apr 15;6(4):102047.  [Abstract]

    C57BL/6J wild-type mice were fed FPC diet for 27 weeks. Drugs were administered from 19 to 27 weeks. 8 mg/kg of APB-R3 (SAFA-hIL-18BP) was intraperitoneally administered three times a week as indicated. 5 mg/kg of THRβ agonist (MGL-3196; Resmetirom) was daily orally gavaged as compared group. Representative images of H&E liver sections.

    Resmetirom purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2025 Apr 15;6(4):102047.  [Abstract]

    C57BL/6J wild-type mice were fed FPC diet for 27 weeks. Drugs were administered from 19 to 27 weeks. 8 mg/kg of APB-R3 (SAFA-hIL-18BP) was intraperitoneally administered three times a week as indicated. 5 mg/kg of THRβ agonist (MGL-3196; Resmetirom) was daily orally gavaged as compared group. ELISA assay was conducted to measure plasma Pro-C3.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Resmetirom (MGL-3196) is a highly selective and orally active thyroid hormone receptor β (THR-β) agonist with an EC50 value of 0.21 μM. Resmetirom can be used for the study of noncirrhotic nonalcoholic steatohepatitis[1].

    IC50 & Target

    EC50: 0.21 μM (THR-β)[1]

    Cellular Effect
    Cell Line Type Value Description References
    Huh-7 EC50
    303 nM
    Compound: 4
    Effect on CPT1A gene expression in human Huh-7 cells measured for 24 hrs
    Effect on CPT1A gene expression in human Huh-7 cells measured for 24 hrs
    [PMID: 39221768]
    In Vitro

    Resmetirom (MGL-3196) is 28-fold selective for THR-β (EC50=0.21 μM) over THR-α (EC50=3.74 μM ) in a functional assay. Resmetirom (MGL-3196) shows an IC20 of roughly 30 μM for blockage of the hERG channel. The IC50 for CYP3A4/5 and for CYP2C19 is >50 μM, and there is only weak inhibition (roughly 22 μM) of CYP2C9[1].

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

    In Vivo

    Resmetirom (MGL-3196) exhibits good exposures and reasonable oral bioavailability in rats. The volume of distribution and clearance are both low. Dose proportional increases in exposure are observed for a suspension of Resmetirom (MGL-3196) given orally to DIO mice[1].In animals treated with Resmetirom (MGL-3196) there is a reduction in cholesterol and in liver size, which is secondary to reduction of liver TG. There is no effect on bone mineral density (BMD) or heart or kidney size in Resmetirom (MGL-3196) treated animals[1].

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

    Clinical Trial
    Molecular Weight

    435.22

    Formula

    C17H12Cl2N6O4

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    N#CC1=NN(C2=CC(Cl)=C(OC(C=C3C(C)C)=NNC3=O)C(Cl)=C2)C(NC1=O)=O

    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 : 70 mg/mL (160.84 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 2.2977 mL 11.4884 mL 22.9769 mL
    5 mM 0.4595 mL 2.2977 mL 4.5954 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
    ×
    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: ≥ 3.75 mg/mL (8.62 mM); Clear solution

      This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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: ≥ 3.75 mg/mL (8.62 mM); Clear solution

      This protocol yields a clear solution of ≥ 3.75 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (37.5 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: 99.93%

    References
    Animal Administration
    [1]

    Rats[1]
    Resmetirom (MGL-3196), compounds 54 and 55 are formulated in 4% DMSO, 15% PEG-400, and 81% of 30% HPBCD in phosphate buffer and are administered intraperitoneally. For MGL-3196 and 54, 4 rats per group are tested at 5, 20, and 37.5 mg/kg. For 55, 3 rats per group are tested at 5 and 15 mg/kg and 4 rats are tested at 50 mg/kg[1].

    Mice[1]
    Six week old C57Bl/6J mice are placed on a high fat diet for 34 weeks. At day 0, 9 mice per group are treated daily doses by gavage with vehicle (2% Klucel LF, 0.1% Tween 80 in water) or 0.3, 1, 3, or 10 mg/kg Resmetirom (MGL-3196) for 23 days. In a parallel study, at day 0, 9 mice per group are treated with daily doses of vehicle (Dulbecco’s phosphate buffered saline, pH adjusted to 9.0 with 1 N NaOH) or 10, 30, or 100 μg/kg T3[1].

    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 2.2977 mL 11.4884 mL 22.9769 mL 57.4422 mL
    5 mM 0.4595 mL 2.2977 mL 4.5954 mL 11.4884 mL
    10 mM 0.2298 mL 1.1488 mL 2.2977 mL 5.7442 mL
    15 mM 0.1532 mL 0.7659 mL 1.5318 mL 3.8295 mL
    20 mM 0.1149 mL 0.5744 mL 1.1488 mL 2.8721 mL
    25 mM 0.0919 mL 0.4595 mL 0.9191 mL 2.2977 mL
    30 mM 0.0766 mL 0.3829 mL 0.7659 mL 1.9147 mL
    40 mM 0.0574 mL 0.2872 mL 0.5744 mL 1.4361 mL
    50 mM 0.0460 mL 0.2298 mL 0.4595 mL 1.1488 mL
    60 mM 0.0383 mL 0.1915 mL 0.3829 mL 0.9574 mL
    80 mM 0.0287 mL 0.1436 mL 0.2872 mL 0.7180 mL
    100 mM 0.0230 mL 0.1149 mL 0.2298 mL 0.5744 mL
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    • 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.

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