Resmetirom

SKU: orb1304018

Description

Resmetirom (MGL-3196) is an orally active, highly selective thyroid hormone receptor-beta (THR-β) agonist with an EC50 of 0.21 μM. It is a research compound used in studies of non-alcoholic steatohepatitis (NASH), with applications in both in vitro mechanistic studies and in vivo models of liver disease.

Research Area

Metabolism Research

Key Properties

• CAS Number: 920509-32-6
• MW: 435.22
• Purity: 99.91%
• Formula: C₁₇H₁₂Cl₂N₆O₄
• SMILES: CC(C)c1cc(Oc2c(Cl)cc(cc2Cl)-n2nc(C#N)c(=O)[nH]c2=O)n[nH]c1=O
• Target: Thyroid hormone receptor(THR)
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:3.3 mg/mL (7.58 mM);DMSO:101 mg/mL (232.07 mM)

Bioactivity

• Target IC50:
  THRα:3.74 μM (EC50)|CYP2C9:22 μM|ERG (human):30 μM|THRβ:0.21 μM (EC50)
• In Vivo:
  METHODS: To stud the effect of Resmetirom o the liver the suspension of MGL-3196 (0.3, 1, 3, 10 mg/kg) was administered by gavage to DIO mice for 23 consecutive days. Results: Resmetirom demonstrated good exposure and reasonable oral bioavailability in rats. Bot the distribution volume an the clearance rate are relatively low. Fo the MGL-3196 suspension orally administered to DIO mice, an increased exposure in the dose ratio was observed. Amon the animals treated with McL-3196, both cholesterol and liver size decreased, which was mainly due to the reduction of triglycerides in the liver. Amon the animals treated with McL-3196, there was no effect on bone mineral density (BMD), heart or kidney size. METHODS: To stud the improvement of liver pathological characteristics by Resmetirom, mouse models of non-alcoholic steatohepatitis (NASH) were treated with Resmetirom(3 mg/kg, 5 mg/kg). Results: in the NASH mouse model, Resmetirom was able to significantly improv the pathological characteristics o the liver. Throug the oil red O staining experiment, it was found that Resmetirom could effectively reduce liver fat accumulation, an the effect was more obvious in the high-dose group (5 mg/kg). In addition, Resmetirom can also improve liver fibrosis and inflammation caused by NASH by restorin the expression of RGS5 and inhibitin the activation of STAT3 and NF-κB signaling pathways.
• In Vitro:
  METHODS: CYP3A4/5, CYP2C19 and CYP2C9 were treated with Resmetirom to detec the Inhibition of cell growth. Results the IC50 of ResmetiromCYP3A4/5 and CYP2C19 were both greater than 50 μM, with no growth inhibitory effect the inhibitory effect on CYP2C9 was relatively weak, an the IC50 was approximately 22 μM.

Storage & Handling

• 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/Shipping at ambient temperature.
• Disclaimer: For research use only

Alternative Names

Inhibitor, MGL3196, MGL-3196, MGL 3196, inhibit, VIA 3196, VIA3196, VIA-3196, Resmetirom, THR-β, THR, Thyroidhormonereceptor, Thyroidhormonereceptor(THR), Thyroid hormone receptor(THR), Thyroid Hormone Receptor, Thyroid hormone receptor

Cas No. 920509-32-6

Compound Identifiers

PubChem CID

15981237