Name | Resmetirom |
Description | Resmetirom (VIA-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist. |
In vitro | Resmetiromis 28-fold selective for THR-β (EC50=0.21 μM) over THR-α (EC50=3.74 μM ) in a functional assay. Resmetiromshows 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]. |
Storage | store at low temperature,store under nitrogen | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
Solubility Information | DMSO : 60 mg/mL (137.86 mM)
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Keywords | Inhibitor | MGL-3196 | Thyroid Hormone Receptor | MGL 3196 | Resmetirom | VIA 3196 | THR | inhibit | VIA3196 |
Inhibitors Related | Propylthiouracil | Liothyronine | L-Thyroxine | L-Thyroxine sodium | 2,2-BIS(2-HYDROXY-5-BIPHENYLYL)PROPANE | DS08210767 | Carbimazole | Methimazole | Liothyronine sodium | 2-Thiouracil | PCO371 | Tiratricol |
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