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  5. Methylthiouracil

Methylthiouracil  (Synonyms: MTU)

Cat. No.: HY-B0513 Purity: ≥98.0%
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Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.

For research use only. We do not sell to patients.

Methylthiouracil Chemical Structure

Methylthiouracil Chemical Structure

CAS No. : 56-04-2

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10 mM * 1 mL in DMSO
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100 mg USD 106 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Methylthiouracil:

Methylthiouracil Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Methylthiouracil

View All NF-κB Isoform Specific Products:

View All Isoforms
NF-κB NF-κB1/p50 RelA/p65 RelB c-Rel

View All TNF Receptor Isoform Specific Products:

View All Isoforms
TNFRSF1A/CD120a TNFRSF5/CD40 TNFRSF6/Fas/CD95 TNFRSF8/CD30 TNFRSF9/4-1BB/CD137 TNFRSF16/NGF Receptor/CD271 TNFRSF18/GITR/CD357

View All Interleukin Related Isoform Specific Products:

View All Isoforms
IL-1 IL-2 IL-3 IL-4 IL-5 IL-6 IL-8 IL-10 IL-12 IL-13 IL-15 IL-17 IL-23 IL-7 IL-33 IL-22

View All ERK Isoform Specific Products:

View All Isoforms
ERK ERK1 ERK2 ERK5 ERK8

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.

IC50 & Target[1]

NF-κB

 

IL-6

 

ERK1

 

ERK2

 

In Vitro

HUVECs are treated with various concentrations of MTU (0-20 μM) for 6 h after the addition of LPS (100 ng/mL) for 4 h. MTU inhibits LPS-mediated hyperpermeability in endothelial cells, with the optimal effect occurring at a concentration above 5 μM. The effects of MTU are examined on HUVEC actin cytoskeletal arrangement by immunofluorescence staining of HUVEC monolayers with F-actin labeled fluorescein phalloidin. Control HUVECs exhibit a random distribution of F-actin throughout the cells, with some localization of actin filament bundles at the cell boundaries. Barrier disruption by LPS (100 ng/mL) is manifested by the formation of paracellular gaps in HUVECs. In addition, post-treatment with MTU (10 or 20 μM) results in inhibited formation of LPS-induced paracellular gaps with the formation of dense F-actin rings. To test the cytotoxicity of MTU, cellular viability assays are performed in HUVECs treated with MTU for 24 h. At concentrations up to 20 μM, MTU does not affect cell viability[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Methylthiouracil Related Antibodies
In Vivo

After a single oral administration of Amiodarone to rats, its pharmacokinetic characteristics include: the absorption half-life is approximately 1.83 hours, the elimination half-life ranges from 15 hours (at a dose of 100 mg/kg) to 105 hours (at a dose of 200 mg/kg), and the average oral bioavailability is 39%. Amiodarone is primarily distributed in the lungs, liver, thyroid gland, and adipose tissue, with notably higher drug concentrations in the lungs and adipose tissue compared to other tissues. Following chronic oral administration, Amiodarone shows a significant increase in accumulation in adipose tissue.
Amiodarone can be used for animal modeling to construct pulmonary toxicity models and liver injury models [3][4][5].

Inducing Neurological Defects[3]

Background
Methylthiouracil is an antithyroid drug that inhibits thyroid function, thereby disrupting the central nervous system[1].
Specific Mmodeling Methods
Rat: albino • male and female
Administration: 0.05-0.2 mL • sc • once daily, details of the dosing method are provided in the note
Note
Methylthiouracil Administration Method: Methylthiouracil is suspended in a 2% sodium alginate (HY-Y1310A) solution at a concentration of 4%.
(1) . From 0-10 days after birth, 0.05 mL of the suspension is administered via subcutaneous injection;
(2) . From 10-20 days after birth, 0.1 mL of the suspension is administered via subcutaneous injection;
(3) . From 20-24 days after birth, 0.2 mL of the suspension is administered via subcutaneous injection.
Modeling Indicators
Phenotypic Observations: Rats exhibited decreased body weight, reduced brain weight, slower growth rate, and diminished responsiveness to external stimuli.
Histological Changes: In the cerebral cortex of the rats, the volume of pyramidal cells decreased, their number increased, and the supportive or structural substance (intercellular matrix) between neurons in the cerebral cortex decreased during the rats' development.
Correlated Product(s): Sodium alginate (Viscosity 200±20mpa.s) (HY-Y1310A)
Opposite Product(s): /

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Molecular Weight

142.18

Formula

C5H6N2OS
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(C=C(C)N1)NC1=S
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (351.67 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 7.0333 mL 35.1667 mL 70.3334 mL
5 mM 1.4067 mL 7.0333 mL 14.0667 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

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Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (17.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% Corn Oil

    Solubility: ≥ 2.5 mg/mL (17.58 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References
Cell Assay
[1]

MTT is used as an indicator of cell viability. Primary human umbilical vein endothelial cells (HUVECs) are grown in 96-well plates at a density of 5×103 cells/well. After 24 h, the cells are washed with fresh medium and treated with MTU (0-20 μM). After a 48 h incubation period, the cells are washed, and 100 μL of MTT (1 mg/mL) is added, followed by incubation for 4 h. Finally, DMSO (150 μL) is added to solubilize the formazan salt formed, and the amount of formazan salt is determined by measuring the OD at 540 nm using a microplate reader [1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[1]

Mice[1]
Male C57BL/6 mice (6-7 weeks old; average weight, 27 g) are used in this study. Mice are administered LPS (0.3 mg/mouse or 15 mg/kg, intravenously). After 4 h, the mice are intravenously treated with MTU (142 or 284 μg/kg, for 6 h) and injected with 1% Evans blue dye solution in normal saline. Six hours later, the mice are sacrificed and peritoneal exudates are collected by washing cavities with 5 mL of normal saline and by centrifuging at 200× g for 10 min. The absorbance of the supernatant is read at 650 nm. Vascular permeabilities are expressed as μg of dye/mouse that leaked into the peritoneal cavity and are determined using a standard curve.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 7.0333 mL 35.1667 mL 70.3334 mL 175.8335 mL
5 mM 1.4067 mL 7.0333 mL 14.0667 mL 35.1667 mL
10 mM 0.7033 mL 3.5167 mL 7.0333 mL 17.5833 mL
15 mM 0.4689 mL 2.3444 mL 4.6889 mL 11.7222 mL
20 mM 0.3517 mL 1.7583 mL 3.5167 mL 8.7917 mL
25 mM 0.2813 mL 1.4067 mL 2.8133 mL 7.0333 mL
30 mM 0.2344 mL 1.1722 mL 2.3444 mL 5.8611 mL
40 mM 0.1758 mL 0.8792 mL 1.7583 mL 4.3958 mL
50 mM 0.1407 mL 0.7033 mL 1.4067 mL 3.5167 mL
60 mM 0.1172 mL 0.5861 mL 1.1722 mL 2.9306 mL
80 mM 0.0879 mL 0.4396 mL 0.8792 mL 2.1979 mL
100 mM 0.0703 mL 0.3517 mL 0.7033 mL 1.7583 mL
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Methylthiouracil Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Methylthiouracil56-04-2MTUNF-κBTNF ReceptorInterleukin RelatedERKNuclear factor-κBNuclear factor-kappaBTumor Necrosis Factor ReceptorTNFRILExtracellular signal regulated kinasesInhibitorinhibitorinhibit

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