MGL-3196
(Synonyms: MGL-3196; VIA-3196) 目录号 : GC18243
MGL-3196是一种高选择性的口服甲状腺激素受体β（THRβ）激动剂，EC50为0.21μM。
Cas No.:920509-32-6
Sample solution is provided at 25 µL, 10mM.
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MGL-3196 is a highly selective and orally active thyroid hormone receptor β (THRβ) agonist with an EC50 value of 0.21μM[1]. THRβ is a nuclear receptor that plays a key role in regulating metabolism, growth, and development by binding to thyroid hormones and modulating gene expression[2]. MGL-3196 can be used for the study of nonalcoholic steatohepatitis and cardiovascular diseases[3][4].
In vitro, treatment of HEK-1B1 cells with MGL-3196 (6μM; 48h) significantly induced the expression of THRβ target genes like KLF9 and PCK1 and enhanced mitochondrial respiration[5].
In vivo, MGL-3196 (3mg/kg/day; gavage; 8 weeks) reduced liver weight, circulating triglycerides and total cholesterol, and improved histological signs of steatosis and fibrosis in SPF mice fed a MASH diet[6]. MGL-3196 (1mg/kg/day; orally; 8 weeks) significantly reduced liver weight, improved histological steatosis and lobular inflammation scores, and lowered plasma cholesterol and alanine transaminase (ALT) levels in a mouse model of fatty liver disease induced by the GAN diet[7].
References:
[1] Kelly MJ, Pietranico-Cole S, Larigan JD, 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;57(10):3912-3923.
[2] Mullur R, Liu YY, Brent GA. Thyroid hormone regulation of metabolism. Physiol Rev. 2014;94(2):355-382.
[3] Keam SJ. Resmetirom: First Approval. Drugs. 2024;84(6):729-735.
[4] Zisis M, Chondrogianni ME, Androutsakos T, et al. Linking Cardiovascular Disease and Metabolic Dysfunction-Associated Steatotic Liver Disease (MASLD): The Role of Cardiometabolic Drugs in MASLD Treatment. Biomolecules. 2025;15(3):324.
[5] Hones GS, Sivakumar RG, Hoppe C, König J, Führer D, Moeller LC. Cell-Specific Transport and Thyroid Hormone Receptor Isoform Selectivity Account for Hepatocyte-Targeted Thyromimetic Action of MGL-3196. Int J Mol Sci. 2022;23(22):13714.
[6] Zhang YH, Xie R, Dai CS, et al. Thyroid hormone receptor-beta agonist HSK31679 alleviates MASLD by modulating gut microbial sphingolipids. J Hepatol. 2025;82(2):189-202.
[7] Zhou M, Li C, Byrne FL, et al. Beneficial effects of MGL-3196 and BAM15 combination in a mouse model of fatty liver disease. Acta Physiol (Oxf). 2024;240(10):e14217.
MGL-3196是一种高选择性的口服甲状腺激素受体β（THRβ）激动剂，EC50为0.21μM[1]。THRβ是一种核受体，通过与甲状腺激素结合并调节基因表达，在代谢、生长和发育中发挥关键作用[2]。MGL-3196可用于研究非酒精性脂肪性肝炎（NASH）和心血管疾病[3][4]。
在体外实验中，用6μM的MGL-3196处理HEK-1B1细胞48小时，显著诱导了THRβ靶基因（如KLF9和PCK1）的表达，并增强了线粒体呼吸[5]。
在体内实验中，MGL-3196（3mg/kg/天；灌胃给药；持续8周）降低了喂食MASH饮食的SPF小鼠的肝脏重量，减少了循环中的甘油三酯和总胆固醇水平，并改善了脂肪肝和纤维化的组织学表现[6]。在由GAN饮食诱导的脂肪肝小鼠模型中，MGL-3196（1mg/kg/天； 口服给药；持续8周）显著降低了肝脏重量，改善了脂肪肝和小叶炎症的组织学评分，并降低了血浆胆固醇和丙氨酸转氨酶（ALT）水平[7]。
| Cell experiment [1]: | |
Cell lines | HEK-1B1 cells |
Preparation Method | HEK-1B1 cells were maintained in a DMEM containing 4.5g/L glucose, 1% pyruvate (DMEM+GlutaMAX), 1% ZellShield, and 10% FCS supplemented with 800µg/mL G418. Only those cells in a passage number below 7 were used for the experiments. MGL-3196 were dissolved in DMSO at a concentration of 10mM. 8×105 HEK-1B1 cells were seeded in a 6-well dish and grown to 60-80% confluence overnight. After 24h in the TH-depleted medium, HEK-1B1 cells were treated with MGL-3196 (6μM) or DMSO (control) for another 48h. The total RNA was extracted for gene expression analysis. The oxygen consumption rate (OCR) was measured with an XF24 extracellular analyzer. |
Reaction Conditions | 6μM; 48h |
Applications | Treatment of HEK-1B1 cells with MGL-3196 significantly induced the expression of THRβ target genes like KLF9 and PCK1 and enhanced mitochondrial respiration. |
| Animal experiment [2]: | |
Animal models | C57BL/6 SPF mice |
Preparation Method | C57BL/6 SPF mice (6-week-old) were housed in rigid autoclaved cages (6 per cage) under a 12-h light-dark cycle. All mice were firstly fed with a MASH diet containing 21.1% kcal fat, 1.25% kcal cholesterol and 41.0% kcal sucrose by a sugar water solution of 23.1g/L d-fructose and 18.9g/L d-glucose for 16 weeks to induce MASH. For in vivo experiments, each group of the above MASH mice were directly gavaged with 3mg/kg MGL-3196 (daily, the same volume of saline as the solvent control) for 8 weeks. Their body weights and food intake were monitored weekly. Their fecal samples were collected for metagenomic and metabonomic analysis. Ultimately, all mice were euthanized by exsanguination to collect their colonic, serum and hepatic samples to determine serological, standard H&E, Sirius red staining and Oil red O histological analysis, respectively. |
Dosage form | 3mg/kg/day; gavage; 8 weeks |
Applications | MGL-3196 reduced liver weight, circulating triglycerides and total cholesterol, and improved histological signs of steatosis and fibrosis in SPF mice fed a MASH diet. |
References: | |
| Cas No. | 920509-32-6 | SDF | |
| 别名 | MGL-3196; VIA-3196 | ||
| 化学名 | 2-[3,5-dichloro-4-[[1,6-dihydro-5-(1-methylethyl)-6-oxo-3-pyridazinyl]oxy]phenyl]-2,3,4,5-tetrahydro-3,5-dioxo-1,2,4-triazine-6-carbonitrile | ||
| Canonical SMILES | O=C(N1)N(C2=CC(Cl)=C(OC3=NNC(C(C(C)C)=C3)=O)C(Cl)=C2)N=C(C#N)C1=O | ||
| 分子式 | C17H12Cl2N6O4 | 分子量 | 435.2 |
| 溶解度 | DMF: 20 mg/ml,DMSO: 20 mg/ml,Ethanol: 1 mg/ml | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2978 mL | 11.489 mL | 22.9779 mL |
| 5 mM | 459.6 μL | 2.2978 mL | 4.5956 mL |
| 10 mM | 229.8 μL | 1.1489 mL | 2.2978 mL |
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| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
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| % DMSO % % Tween 80 % saline | ||||||||||
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计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
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2.
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Quality Control & SDS
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- Purity: >99.50%
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