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  3. Resmetirom

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

Cat. No.: HY-12216 Purity: 99.71%
Handling Instructions

Resmetirom (MGL-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist with an EC50 value of 0.21 μM.

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

Resmetirom Chemical Structure

Resmetirom Chemical Structure

CAS No. : 920509-32-6

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10 mM * 1 mL in DMSO USD 105 In-stock
Estimated Time of Arrival: December 31
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10 mg USD 160 In-stock
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50 mg USD 440 In-stock
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100 mg USD 750 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

Resmetirom (MGL-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist with an EC50 value of 0.21 μM.

IC50 & Target

EC50: 0.21 μM (THR-β)[1]

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].

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].

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.
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: 

DMSO : ≥ 31 mg/mL (71.23 mM)

*"≥" means soluble, but saturation unknown.

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
10 mM 0.2298 mL 1.1488 mL 2.2977 mL
*Please refer to the solubility information to select the appropriate solvent.
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

Purity: 99.71%

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Resmetirom
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HY-12216
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