|2-(3,5-二氯-4-((5-异丙基-6-氧代-1,6-二氢哒嗪-3-基)氧基)苯基)-3,5-二氧代-2,3,4,5-四氢-1,2,4-三嗪-6-腈|CsnPharm

CAS No.: 920509-32-6

2-(3,5-Dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile Catalog No. CSN19099

Synonyms: MGL-3196;VIA-3196

MGL-3196 is a selective thyroid hormone receptor β agonist with EC50s of 0.21 and 3.74 µM for TRβ and TRα respectively.

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靶点选择性

生物活性

实验方案

技术信息

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]

动物研究

剂量

Rat: 5 mg/kg - 37.5 mg/kg^[1] (i.p.) Mice: 0.3 mg/kg - 10 mg/kg^[1] (p.o.)

给药途径

i.p., p.o.

动物药代数据

Animal	Rats^[1]
Dose	5 mg/kg
Administration	i.v. or p.o.
F	45% (p.o.)
T_1/2	3.4 h (i.v.) 4.08 h (p.o.)
T_max	6 h (p.o.)
CL	2.35 ml/min/kg (i.v.)
C_max	1.71 μg/h (p.o.)
Vss	0.422 l/kg (i.v.)
AUC	38.1 μg·h/ml (i.v.) 17.4 μg·h/ml (p.o.)

临床研究

NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
NCT02912260	Non-alcoholic Steatohepatitis	Phase 2	Active, not recruiting	April 2018	-
NCT02542969	Healthy	Phase 1	Completed	-	United States, Arizona ... more >> Celerion Tempe, Arizona, United States, 85283 Collapse <<
NCT03038022	Heterozygous Familial Hypercho... more >>lesterolemia Collapse <<	Phase 2	Completed	-	Denmark ... more >> Madrigal Research Site Aalborg, Denmark Madrigal Research Site Viborg, Denmark Collapse <<

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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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.2977 mL
- 11.4884 mL
- 22.9768 mL
- 5 mM
- 0.4595 mL
- 2.2977 mL
- 4.5954 mL
- 10 mM
- 0.2298 mL
- 1.1488 mL
- 2.2977 mL

技术信息

CAS号

920509-32-6

储存条件

粉末: Inert atmosphere,Store in freezer, under -20°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C17H12Cl2N6O4

运输

蓝冰

分子量

435.22

别名

MGL-3196;VIA-3196

溶解度

DMSO	34.0 mg/mL (78.1 mM)
Water	insoluble

动物实验配方

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2-(3,5-Dichloro-4-((5-isopropyl-6-oxo-1,6-dihydropyridazin-3-yl)oxy)phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile Catalog No. CSN19099

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