An agonist of TRβ
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Resmetirom

Item No. 23845

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
2-[3,5-dichloro-4-[[1,6-dihydro-5-(1-methylethyl)-6-oxo-3-pyridazinyl]oxy]phenyl]-2,3,4,5-tetrahydro-3,5-dioxo-1,2,4-triazine-6-carbonitrile
CAS Number
920509-32-6
Synonyms
  • ​MGL-3196
  • VIA-3196
Molecular Formula
C17H12Cl2N6O4
Formula Weight
435.2
Purity
≥95%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
λmax
306 nm
SMILES
O=C(N1)N(C2=CC(Cl)=C(OC3=NNC(C(C(C)C)=C3)=O)C(Cl)=C2)N=C(C#N)C1=O
InChi Code
InChI=1S/C17H12Cl2N6O4/c1-7(2)9-5-13(22-23-15(9)26)29-14-10(18)3-8(4-11(14)19)25-17(28)21-16(27)12(6-20)24-25/h3-5,7H,1-2H3,(H,23,26)(H,21,27,28)
InChi Key
FDBYIYFVSAHJLY-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

    $31

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    5 mg

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    10 mg

    $154

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    25 mg

    $270

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    Cayman Chemical
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    OBESITY RESEARCH SOLUTIONS
    Product Description

    Resmetirom is an agonist of thyroid hormone receptor β (TRβ; EC50s = 0.21 and 3.74 µM for TRβ and TRα, respectively).1 It also inhibits ether-a-go-go-related gene (ERG) potassium channels (IC50 = 30 µM). Resmetirom is a liver-directed compound, with a liver to plasma ratio of 8:1 in mice with diet-induced obesity (DIO), which reduces the likelihood of adverse effects from systemic exposure. It does not affect the expression of α-myosin heavy chain (α-MHC) in a rat model of hypothyroidism, an effect mediated by TRα, indicating low potential for cardiac adverse effects. Resmetirom lowers non-HDL cholesterol and liver triglycerides without affecting thyroid stimulating hormone (Tsh) levels in rat and rabbit models of hypercholesterolemia. It also lowers plasma glucose levels and improves insulin sensitivity in DIO mice.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Kelly, M.J., Pietranico-Cole, S., Larigan, J.D., et al. Discovery of 2-[3,5-dichloro-4-(5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yloxy)phenyl]-3,5-dioxo-2,3,4,5-tetrahydro[1,2,4]triazine-6-carbonitrile (MGL-3196), a highly selective thyroid hormone receptor β agonist in clinical trials for the treatment of dyslipidemia. J. Med. Chem. 57(10), 3912-3923 (2014).