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Methimazole

Name: Methimazole
Brand: TargetMol
SKU: T0840
Price: 30 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T0840Cas No. 60-56-0

Alias Thiamazole, Tapazole

Methimazole (Thiamazole) is an antithyroid compound with significant hepatotoxicity and is often used in the study of hyperthyroidism.

Methimazole

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Purity: 99.59%

Catalog No. T0840Alias Thiamazole, TapazoleCas No. 60-56-0

Methimazole (Thiamazole) is an antithyroid compound with significant hepatotoxicity and is often used in the study of hyperthyroidism.

Pack Size	Price	USA Warehouse	Global Warehouse
200 mg	$30	In Stock	In Stock
500 mg	$44	In Stock	In Stock
1 g	$56	-	In Stock
1 mL x 10 mM (in DMSO)	$39	In Stock	In Stock

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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]

All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.

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Batch Information

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Purity:99.59%

Appearance:Solid

Color:White

Resource Download

COA LCMS HPLC HNMR

Product Introduction

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

Bioactivity

Description	Methimazole (Thiamazole) is an antithyroid compound with significant hepatotoxicity and is often used in the study of hyperthyroidism.
Synonyms	Thiamazole, Tapazole

Chemical Properties

Molecular Weight	114.17
Formula	C₄H₆N₂S
Cas No.	60-56-0
Smiles	CN1C=CN=C1S
Relative Density.	1.176 g/cm3 (Estimated)

Storage & Solubility Information

Storage

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

Solubility Information

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.

In Vivo Formulation

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

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

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

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments

and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent

10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO TargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO TargetMol | reagent stock solution to 400 μL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH₂O TargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

You can also refer to dose conversion for different animals. More Dose Conversion

Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc