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Resmetirom

Resmetirom structure

CAS No:
920509-32-6
Formula:
C17H12Cl2N6O4
Chemical Name:
Resmetirom
Synonyms:
Resmetirom (MGL-3196,VIA-3196);MGL-3196; MGL 3196; MGL3196; VIA-3196; VIA3196; VIA-3196;VIA3196;VIA-3196;MGL-3196;Resmetirom;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;CS-2429
Categories:
Pharmaceutical Intermediates > Bulk Drug Intermediates

Description

MGL-3196 has been used in trials studying the treatment of Non-alcoholic steatohepatitis and Heterozygous Familial Hypercholesterolemia.

MGL-3196 is an agonist of thyroid hormone receptor β (TRβ; EC50s = 0.21 and 3.74 μM for TRβ and TRα, respectively). It also inhibits ether-a-go-go-related gene (ERG) potassium channels (IC50= 30 μM). MGL-3196 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. MGL-3196 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. Formulations containing MGL-3196 are in clinical trials for the treatment of non-alcoholic steatohepatitis (NASH) and familial hypercholesterolemia.

Resmetirom Basic Attributes

Molecular Weight：

435.22

Exact Mass：

434.0297083

UNII：

RE0V0T1ES0

Color/Form：

Yellow to orange

Characteristics

Density：

1.65±0.1 g/cm3(Predicted)

PKA：

3.96±0.40(Predicted)

Critical Temperature & Pressure：

Inert atmosphere,Store in freezer, under -20°C

Drug Information

MeSH Entry Terms：

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

Resmetirom Use and Manufacturing

Resmetirom (MGL-3196) is a liver-directed, orally active, selective thyroid hormone receptor-beta agonist. It works by blocking the formation of fat in the liver and can be used to treat non-alcoholic steatohepatitis (NASH).

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