Resmetirom

SKU: orb1304018

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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

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Key Properties

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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

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Target IC50	THRα:3.74 μM (EC50)\|CYP2C9:22 μM\|ERG (human):30 μM\|THRβ:0.21 μM (EC50)
In Vivo	METHODS: To study the effect of Resmetirom on 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. Both the distribution volume and the clearance rate are relatively low. For the MGL-3196 suspension orally administered to DIO mice, an increased exposure in the dose ratio was observed . Among the animals treated with McL-3196, both cholesterol and liver size decreased, which was mainly due to the reduction of triglycerides in the liver. Among the animals treated with McL-3196, there was no effect on bone mineral density (BMD), heart or kidney size . METHODS: To study 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 improve the pathological characteristics of the liver. Through the oil red O staining experiment, it was found that Resmetirom could effectively reduce liver fat accumulation, and 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 restoring the expression of RGS5 and inhibiting the activation of STAT3 and NF-κB signaling pathways. Read more...
In Vitro	METHODS: CYP3A4/5, CYP2C19 and CYP2C9 were treated with Resmetirom to detect 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, and the IC50 was approximately 22 μM. Read more...

Storage & Handling

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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.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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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

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Cas No. 920509-32-6

Compound Identifiers

PubChem CID

15981237 ↗

Key Properties

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No computed properties available.

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Purity:	>98% (HPLC)
CAS Number:	920509-32-6
MW:	435.2
Formula:	C₁₇H₁₂Cl₂N₆O₄

Resmetirom

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Research Area

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Key Properties

Bioactivity

Storage & Handling

Alternative Names

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