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Resmetirom

Catalog No. T3595   CAS 920509-32-6
Synonyms: VIA-3196, MGL3196

Resmetirom (VIA-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist.

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Resmetirom Chemical Structure
Resmetirom, CAS 920509-32-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 33.00
2 mg In stock $ 47.00
5 mg In stock $ 89.00
10 mg In stock $ 128.00
25 mg In stock $ 225.00
50 mg In stock $ 360.00
100 mg In stock $ 535.00
500 mg In stock $ 1,190.00
1 mL * 10 mM (in DMSO) In stock $ 84.00
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Purity: 100%
Purity: 99.13%
Purity: 99.05%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Resmetirom (VIA-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist.
Targets&IC50 THRβ:0.21 μM(EC50)
In vitro MGL-3196 is 28-fold selective for THR-β (EC50=0.21 μM) over THR-α (EC50=3.74 μM ) in a functional assay. 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].
In vivo MGL-3196 demonstrates favorable exposures and acceptable oral bioavailability in rats, with both the volume of distribution and clearance being low. When administered orally to DIO mice, MGL-3196 in a suspension form shows dose-dependent increases in exposure[1]. Treatment with MGL-3196 leads to decreased cholesterol levels and liver size, attributed to the reduction of liver triglycerides (TG). Importantly, no impact is observed on bone mineral density (BMD), or the size of the heart or kidneys in animals receiving MGL-3196[1].
Synonyms VIA-3196, MGL3196
Molecular Weight 435.22
Formula C17H12Cl2N6O4
CAS No. 920509-32-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 31 mg/mL

TargetMolReferences and Literature

1. Kelly, M., Pietranico-Cole, S., Larigan, J., Haynes, N., Reynolds, C., & Scott, N. et al. (2014). 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. Journal Of Medicinal Chemistry, 57(10), 3912-3923. doi: 10.1021/jm4019299

Related compound libraries

This product is contained In the following compound libraries:
Drug Repurposing Compound Library Bioactive Compounds Library Max Nuclear Receptor Compound Library Bioactive Compound Library Anti-Cardiovascular Disease Compound Library NO PAINS Compound Library Endocrinology-Hormone Compound Library Clinical Compound Library Immunology/Inflammation Compound Library ReFRAME Related Library

Related Products

Related compounds with same targets
L-Thyroxine NH-3 Carbimazole Protirelin Acetate(24305-27-9 free base) KAT681 3,5-Diiodo-L-thyronine Liothyronine Triiodothyronine Sulfate

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Keywords

Resmetirom 920509-32-6 Endocrinology/Hormones Thyroid hormone receptor(THR) VIA-3196 Inhibitor MGL-3196 Thyroid Hormone Receptor MGL 3196 VIA 3196 THR inhibit VIA3196 MGL3196 inhibitor

 

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