Resmetirom
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货号：A679714
MGL-3196 is a selective thyroid hormone receptor β agonist with EC50s of 0.21 and 3.74 µM for TRβ and TRα respectively.
Resmetirom 化学结构
Resmetirom 3D分子结构
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Resmetirom 纯度/质量文件 产品仅供科研
货号：A679714
标准纯度：
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Resmetirom 质控信息
Resmetirom 生物活性
描述
MGL-3196 is a highly selective thyroid hormone receptor β agonist with EC50 values of 0.21μM, 28-fold selective for THR-β over THR-α. It is used for research of treatment for Dyslipidemia in clinical trials. Oral administration of MGL-3196 at doses ranging in 0.3-10mg/kg, daily, for 23 days, significantly lowered cholesterol and liver size of diet-induced obese mice, without change in bone mineral density. It showed outstanding safety in a rat heart model and was efficacious in a preclinical model at doses that showed no impact on the central thyroid axis[2]
作用机制
The cyano group in MGL-3196 is accommodated in the active site of THR-β. The cyanoazauracil of MGL-3196 interacts directly with the ARG320 site.[2]
Resmetirom 动物研究
Dose
Rat: 5 mg/kg - 37.5 mg/kg[1] [1]
Administration
i.p., p.o.
Pharmacokinetics
Animal
Rats[1]
Dose
5 mg/kg
Administration
i.v. or p.o.
F
45% (p.o.)
T1/2
3.4 h (i.v.)
Tmax
6 h (p.o.)
CL
2.35 ml/min/kg (i.v.)
Cmax
1.71 μg/h (p.o.)
Vss
0.422 l/kg (i.v.)
AUC
38.1 μg·h/ml (i.v.)
Resmetirom 参考文献
[1] Kelly MJ, Pietranico-Cole S, et al. 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. J Med Chem. 2014 May 22;57(10):3912-23.
[2] Kelly MJ, Pietranico-Cole S, Larigan JD, Haynes NE, Reynolds CH, Scott N, Vermeulen J, Dvorozniak M, Conde-Knape K, Huang KS, So SS, Thakkar K, Qian Y, Banner B, Mennona F, Danzi S, Klein I, Taub R, Tilley J. 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. J Med Chem. 2014 May 22;57(10):3912-23. doi: 10.1021/jm4019299. Epub 2014 Apr 8. PMID: 24712661.
Resmetirom 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.30mL
0.46mL
0.23mL
11.49mL
2.30mL
1.15mL
22.98mL
4.60mL
2.30mL
Resmetirom 技术信息
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