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Methimazole

Name: Methimazole
Brand: TargetMol
SKU: T0840
Price: 138 CNY
Availability: InStock
Rating: 5 (10 reviews)

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很棒

纯度: 99.59%

货号 T0840Cas号 60-56-0

别名 甲巯咪唑, Thiamazole, Tapazole

Methimazole (Thiamazole) 是抗甲状腺化合物，具有显著的肝毒性，常用于研究甲亢。

Methimazole

一键复制产品信息

很棒

纯度: 99.59%

货号 T0840 别名 甲巯咪唑, Thiamazole, TapazoleCas号 60-56-0

Methimazole (Thiamazole) 是抗甲状腺化合物，具有显著的肝毒性，常用于研究甲亢。

规格	价格	库存
50 mg	¥ 138	现货
100 mg	¥ 182	现货
500 mg	¥ 393	现货
1 g	¥ 567	现货
1 mL x 10 mM (in DMSO)	¥ 443	现货

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TargetMol的所有产品仅用作科学研究或药证申报，不能被用于人体，我们不向个人提供产品和服务。请您遵守承诺用途，不得违反法律法规规定用于任何其他用途。

实验操作小课堂

常见问题解答

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纯度: 99.59%

颜色: 白色

性状: Solid

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COA LCMS HPLC HNMR 产品操作手册

产品介绍

Methimazole AI Summary

Methimazole is a versatile inhibitor with a range of bioactivities and specific pharmacokinetic properties. It inhibits Dopamine beta hydroxylase with Ki values of 45,000 nM at pH 4.5 and 716,000 nM at pH 6.6, and an IC50 value of 754,000 nM. Additionally, it inhibits Menin-MLL interaction, Aldehyde Dehydrogenase 1 (ALDH1A1), Bacillus subtilis Sfp phosphopantetheinyl transferase (PPTase), Lamin A splicing, ROR gamma transcriptional activity, JMJD2A-Tudor Domain, Histone Lysine Methyltransferase G9a, and human tyrosyl-DNA phosphodiesterase 1 (TDP1). It also blocks Ebola Virus entry and enhances SMN2 splice variant expression. In terms of pharmacokinetics, it demonstrates a LogD7.4 value of -0.42 and plasma protein binding of approximately 18.64% in rat plasma and 18.99% in human plasma. It shows low potency in inhibiting Bsep/BSEP mediated bile salt export with IC50 values > 1,000,000 nM in rat and human models. The compound displays hepatotoxicity with a high LTKB-BD DILI severity score of 8.0 and a combined HepSE score of 2.0. Methimazole also activates AMPK in rat L6 cells, increasing [3H]dGlc uptake by 93% and has a half-life of 2.4 hours with a clearance of 3.7 mL.min^-1.kg^-1 and a volume of distribution at steady state of 0.86 L.kg^-1 in humans. Notably, it inhibits sodium fluorescein uptake in OATP1B1 and OATP1B3 transfected cells, and displays antioxidant activity with an IC50 of 5,600 nM. The compound exhibits significant antifungal and antibacterial activities and shows antithyroid effects in rats, indicated by decreased thyroid hormone levels. It also inhibits human CYP3A4 and various transport proteins such as MRP2, MRP4, and BSEP with IC50 values > 133,000 nM. Regarding its antiviral properties, compound 421089 shows varying degrees of inhibition against SARS-CoV-2 infected cells and demonstrates weak or no binding affinity towards numerous human receptors and enzymes, with AC50 values > 30,000 nM..

Note: Summary generated by AI. Data source: ChEMBL

生物活性

产品描述	Methimazole (Thiamazole) is an antithyroid compound with significant hepatotoxicity and is often used in the study of hyperthyroidism.
别名	甲巯咪唑, Thiamazole, Tapazole

化学信息

分子量	114.17
分子式	C₄H₆N₂S
CAS No.	60-56-0
Smiles	CN1C=CN=C1S
密度	1.176 g/cm3 (Estimated)

储存&溶解度

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

Ethanol: 22 mg/mL (192.7 mM), Sonication is recommended.

DMSO: 60 mg/mL (525.53 mM), Sonication is recommended.

H2O: 21 mg/mL (183.94 mM), Sonication is recommended.

体内实验配方

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (17.52 mM), Sonication is recommended.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

H2O/Ethanol/DMSO

	1mg	5mg	10mg	50mg
1 mM	8.7589 mL	43.7943 mL	87.5887 mL	437.9434 mL
5 mM	1.7518 mL	8.7589 mL	17.5177 mL	87.5887 mL
10 mM	0.8759 mL	4.3794 mL	8.7589 mL	43.7943 mL
20 mM	0.4379 mL	2.1897 mL	4.3794 mL	21.8972 mL
50 mM	0.1752 mL	0.8759 mL	1.7518 mL	8.7589 mL
100 mM	0.0876 mL	0.4379 mL	0.8759 mL	4.3794 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：

比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10只，您使用的配方为 10% DMSO + 40% PEG300 + 5% Tween 80 + 45% Saline / PBS / ddH₂O，那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 100 μL DMSO （母液浓度为 20 mg/mL ）, 如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法： 取 100 μL DMSO 母液，添加 400 μL PEG300 混匀澄清，再加 50 μL Tween 80, 混匀澄清, 再加 450 μL Saline / PBS / ddH₂O 混匀澄清

以上为“体内实验配液计算器”的使用方法举例，并不是具体某个化合物的推荐配制方式，请根据您的实验动物和给药方式选择适当的溶解方案。

方案所需的各类助溶剂如： DMSO， PEG300， PEG400， Tween 80， SBE-β-CD，玉米油等，均可在TargetMol网站点击购买。

剂量转换

对于不同动物的给药剂量换算，您也可以参考更多

关键词

Thyroidhormonereceptor(THR)Thyroidhormonereceptor Thyroid peripheral conversion Thyroid hormone receptor(THR)Thyroid hormone receptor THR Methimazole Inhibitor inhibit hepatotoxicity hepatocytes cytotoxicity antithyroid

Methimazole

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