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Chemical Structure| 920509-32-6 同义名 : -
CAS号 : 920509-32-6
货号 : A679714
分子式 : C17H12Cl2N6O4
纯度 : 99%
分子量 : 435.22
MDL号 : MFCD26142653
存储条件：

Pure form Inert atmosphere, store in freezer, under -20°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
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]
实验方案
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
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.