Methylthiouracil |
Catalog No.GC16007 |
antithyroid preparation
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1956/4/2
Sample solution is provided at 25 µL, 10mM.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Cell experiment: | 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]. |
Animal experiment: | 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. |
References: [1]. Ku SK, et al. Anti-inflammatory effects of methylthiouracil in vitro and in vivo. Toxicol Appl Pharmacol. 2015 Nov 1;288(3):374-86. |
Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
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].
MTU treatment results in marked inhibition of the peritoneal leakage of dye induced by LPS. The average circulating blood volume for mice is 72 mL/kg. Because the average mouse weight in this study is 27 g, and the average blood volume is 2 mL, the injected MTU (142 or 284 μg/kg) results in a maximum concentration of 10 or 20 μM in the peripheral blood[1].
References:
[1]. Ku SK, et al. Anti-inflammatory effects of methylthiouracil in vitro and in vivo. Toxicol Appl Pharmacol. 2015 Nov 1;288(3):374-86.
Cas No. | 1956/4/2 | SDF | |
Chemical Name | 6-methyl-2-sulfanylidene-1H-pyrimidin-4-one | ||
Canonical SMILES | CC1=CC(=O)NC(=S)N1 | ||
Formula | C5H6N2OS | M.Wt | 142.18 |
Solubility | ≥ 6.65mg/mL in DMSO | Storage | Store at -20°C |
General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. |
Prepare stock solution | |||
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 |
10 mM | 0.7033 mL | 3.5167 mL | 7.0333 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
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