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Resmetirom

(Synonyms: MGL-3196; VIA-3196)

目录号: PL02526 纯度: ≥99%

Resmetirom (MGL-3196) 是高度选择性的THR-β激动剂，EC50值为0.21 μM。

CAS No. :920509-32-6

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中文名称	Resmetirom
中文别名	MGL-3196;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）-3,5-二氧基-2,3,4,5-四氢-1,2,4-三嗪-6-碳腈
英文名称	Resmetirom
英文别名	1,2,4-Triazine-6-carbonitrile,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-;MGL-3196;MGL3196;VIA3196;VIA-3196;Resmetirom;MGL 3196;RE0V0T1ES0;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;Resmetirom [USAN];Resmetirom (USAN/INN);C17H12Cl2N6O4;HMS3746A03;BCP24624;2544AH;BDBM50012905;s6663;WHO 10850;DB12914;SB16825;1,2,4-Triazine-6-carbonitrile, 2-(3,5-dichloro-4-((1,6-dihy;resmétirom;resmetiromum;T6NNVMVJ FCN BR CG EG DO- FT6NMVJ DY1&1;BS-17855;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 (ACI);2-(3,5-dichloro-4-{[6-oxo-5-(propan-2-yl)-1,6-dihydropyridazin-3-yl]oxy}phenyl)-3,5-dioxo-2,3,4,5-tetrahydro-1,2,4-triazine-6-carbonitrile;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;2-[3,5-Dichloro-4-[(5-isopropyl-6-oxo-1H-pyridazin-3-yl]oxy]phenyl]-3,5-dioxo-4H-1,2,4-triazine-6-carbonitrile;2-[3,5-Dichloro-4-[(6-oxo-5-propan-2-yl-1H-pyridazin-3-yl)oxy]phenyl]-3,5-dioxo-1,2,4-triazine-6-carbonitrile
Cas No.	920509-32-6
分子式	C₁₇H₁₂Cl₂N₆O₄
分子量	435.22
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	Resmetirom (MGL-3196) 是高度选择性的THR-β激动剂，EC50值为0.21 μM。

产品详情

Resmetirom (MGL-3196) 是高度选择性的THR-β激动剂，EC₅₀值为0.21 μM。

生物活性

Resmetirom (MGL-3196) is a highly selective thyroid hormone receptor β (THR-β) agonist with an EC 50 value of 0.21 μM.

性状

Solid

IC50 & Target[1][2]

EC50: 0.21 μM (THR-β)

体外研究(In Vitro)

Resmetirom (MGL-3196) is 28-fold selective for THR-β (EC50=0.21 μM) over THR-α (EC50=3.74 μM ) in a functional assay. Resmetirom (MGL-3196) shows an IC20 of roughly 30 μM for blockage of the hERG channel. The IC50 for CYP3A4/5 and for CYP2C19 is >50 μM, and there is only weak inhibition (roughly 22 μM) of CYP2C9. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Resmetirom (MGL-3196) exhibits good exposures and reasonable oral bioavailability in rats. The volume of distribution and clearance are both low. Dose proportional increases in exposure are observed for a suspension of Resmetirom (MGL-3196) given orally to DIO mice.In animals treated with Resmetirom (MGL-3196) there is a reduction in cholesterol and in liver size, which is secondary to reduction of liver TG. There is no effect on bone mineral density (BMD) or heart or kidney size in Resmetirom (MGL-3196) treated animals. has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder -20°C 3 years；4°C 2 years

ClinicalTrial

参考文献

[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

溶解度数据	In Vitro: DMSO : 125 mg/mL (287.21 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

Resmetirom

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