| Name | Resmetirom |
| Description | Resmetirom (MGL-3196) is a THR-β agonist (EC50=0.21 μM), with high selectivity and oral activity. Resmetirom can be used in the research of non-cirrhotic and non-alcoholic steatohepatitis. |
| 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. [1] |
| 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 [1]. 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 [1].
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. [2] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.58 mM), Sonication is recommended.
DMSO : 101 mg/mL (232.07 mM), Sonication is recommended.
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| Keywords | VIA3196 | VIA 3196 | Thyroidhormonereceptor(THR) | Thyroidhormonereceptor | Thyroid hormone receptor(THR) | Thyroid Hormone Receptor | THR-β | THR | Resmetirom | MGL-3196 | MGL 3196 | Inhibitor | inhibit |
| Inhibitors Related | Azetirelin | L-Thyroxine sodium | 2,2-BIS(2-HYDROXY-5-BIPHENYLYL)PROPANE | Iopanoic acid | DS08210767 | Carbimazole | Octinoxate | Methimazole | Posatirelin | PCO371 | Tiratricol | Eneboparatide |
| Related Compound Libraries | Nuclear Receptor Compound Library | FDA-Approved & Pharmacopeia Drug Library | Bioactive Compound Library | ReFRAME Related Library | Toxic Compound Library | Drug Repurposing Compound Library | NO PAINS Compound Library | Anti-Cardiovascular Disease Compound Library | FDA-Approved Drug Library | Immunology/Inflammation Compound Library | Clinical Compound Library | Bioactive Compounds Library Max |
United States
