MGL-3196 | B3010

A selective thyroid hormone receptor β agonist with EC₅₀ values of 0.21 and 3.74 µM for THRβ and THRα, respectively. It significantly lowers non-HDL-C and liver TG in hypercholesterolemic rat and rabbit models at doses where there is no effect on TSH levels or the central thyroid axis. It significantly decreased LDL-C by up to 30%, and showed a statistical trend to reduce TG up to 60% in healthy volunteers, at once daily oral dose of 50 mg or higher for 2 weeks. It does not show THR-α mediated gene expression in a rat heart model indicating low potential for cardiac adverse effects. In vitro assays are predictive of lower off target actions. It shows an IC₂₀ of ~30 μM for blockage of the hERG channel and IC₅₀ >50 μM for CYP3A4/5 and CYP2C19. Formulations containing MGL-3196 are in clinical trials for the treatment of dyslipidemia.

A selective thyroid hormone receptor β agonist with EC₅₀ values of 0.21 and 3.74 µM for THRβ and THRα, respectively. It significantly lowers non-HDL-C and liver TG in hypercholesterolemic rat and rabbit models at doses where there is no effect on TSH levels or the central thyroid axis. It significantly decreased LDL-C by up to 30%, and showed a statistical trend to reduce TG up to 60% in healthy volunteers, at once daily oral dose of 50 mg or higher for 2 weeks. It does not show THR-α mediated gene expression in a rat heart model indicating low potential for cardiac adverse effects. In vitro assays are predictive of lower off target actions. It shows an IC₂₀ of ~30 μM for blockage of the hERG channel and IC₅₀ >50 μM for CYP3A4/5 and CYP2C19. Formulations containing MGL-3196 are in clinical trials for the treatment of dyslipidemia.

B3010 | MGL-3196 DataSheet

Alternate Name/Synonyms: Resmetirom; VIA-3196; 2-[3,5-dichloro-4-[(6-oxo-5-propan-2-yl-1H-pyridazin-3-yl)oxy]phenyl]-3,5-dioxo-1,2,4-triazine-6-carbonitrile; 2-(3,5-dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile; 1,2,4-Triazine-6-carbonitrile; 2-(3,5-dichloro-4-{[6-hydroxy-5-(propan-2-yl)pyridazin-3-yl]oxy}phenyl)-5-hydroxy-3-oxo-2,3-dihydro-1,2,4-triazine-6-carbonitrile

Appearance: Light yellow powder

Formulation:

CAS Number: 920509-32-6

Structure Available?: TRUE

Peptide sequence:

Salt Form: FALSE

Molecular Formula: C₁₇H₁₂Cl₂N₆O₄

Molecular Weight: 435.2

Cell-Permeable?: TRUE

Purity: 0.98

Solubilities: ~20 mg/ml in DMSO and DMF, ~1 mg/ml in Ethanol

Handling: Do not take internally. Wear gloves and mask when handling the product! Avoid contact by all modes of exposure.

Country of Origin: USA

Tag Line: A selective thyroid hormone receptor β agonist

MDL Number: MFCD26142653

PubChem CID: 15981237

SMILES: CC(C)C1=CC(=NNC1=O)OC2=C(C=C(C=C2Cl)N3C(=O)NC(=O)C(=N3)C#N)Cl

InChi: 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