Home>>Signaling Pathways>> Endocrinology and Hormones>> Thyroid hormone Receptor>>MGL-3196

MGL-3196 Sale

(Synonyms: MGL-3196; VIA-3196) 目录号 : GC18243

An agonist of TRβ

MGL-3196 Chemical Structure

Cas No.:920509-32-6

规格 价格 库存 购买数量
1mg 待询 待询
5mg
¥990.00
现货
10mg
¥1,440.00
现货

电话:400-920-5774 Email: sales@glpbio.cn

Customer Reviews

Based on customer reviews.

Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

View current batch:

实验参考方法

Animal experiment:

Rats[1]Resmetirom (MGL-3196), compounds 54 and 55 are formulated in 4% DMSO, 15% PEG-400, and 81% of 30% HPBCD in phosphate buffer and are administered intraperitoneally. For MGL-3196 and 54, 4 rats per group are tested at 5, 20, and 37.5 mg/kg. For 55, 3 rats per group are tested at 5 and 15 mg/kg and 4 rats are tested at 50 mg/kg[1]. Mice[1]Six week old C57Bl/6J mice are placed on a high fat diet for 34 weeks. At day 0, 9 mice per group are treated daily doses by gavage with vehicle (2% Klucel LF, 0.1% Tween 80 in water) or 0.3, 1, 3, or 10 mg/kg Resmetirom (MGL-3196) for 23 days. In a parallel study, at day 0, 9 mice per group are treated with daily doses of vehicle (Dulbecco’s phosphate buffered saline, pH adjusted to 9.0 with 1 N NaOH) or 10, 30, or 100 μg/kg T3[1].

References:

[1]. Kelly MJ, 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.

产品描述

MGL-3196 is an agonist of thyroid hormone receptor β (TRβ; EC50s = 0.21 and 3.74 uM for TRβ and TRα, respectively). It also inhibits ether-a-go-go-related gene (ERG) potassium channels (IC50 = 30 uM). MGL-3196 is a liver-directed compound, with a liver to plasma ratio of 8:1 in mice with diet-induced obesity (DIO), which reduces the likelihood of adverse effects from systemic exposure. It does not affect the expression of α-myosin heavy chain (α-MHC) in a rat model of hypothyroidism, an effect mediated by TRα, indicating low potential for cardiac adverse effects. MGL-3196 lowers non-HDL cholesterol and liver triglycerides without affecting thyroid stimulating hormone (Tsh) levels in rat and rabbit models of hypercholesterolemia. It also lowers plasma glucose levels and improves insulin sensitivity in DIO mice. Formulations containing MGL-3196 are in clinical trials for the treatment of non-alcoholic steatohepatitis (NASH) and familial hypercholesterolemia.

Chemical Properties

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。
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。

溶解性数据

制备储备液
1 mg 5 mg 10 mg
1 mM 2.2978 mL 11.489 mL 22.9779 mL
5 mM 0.4596 mL 2.2978 mL 4.5956 mL
10 mM 0.2298 mL 1.1489 mL 2.2978 mL
  • 摩尔浓度计算器

  • 稀释计算器

  • 分子量计算器

质量
=
浓度
x
体积
x
分子量
 
 
 
*在配置溶液时,请务必参考产品标签上、MSDS / COA(可在Glpbio的产品页面获得)批次特异的分子量使用本工具。

计算

动物体内配方计算器 (澄清溶液)

第一步:请输入基本实验信息(考虑到实验过程中的损耗,建议多配一只动物的药量)
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
第二步:请输入动物体内配方组成(配方适用于不溶于水的药物;不同批次药物配方比例不同,请联系GLPBIO为您提供正确的澄清溶液配方)
% DMSO % % Tween 80 % saline
计算重置