| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
| ln Vitro |
Following a 4-hour addition of LPS (100 ng/mL), HUVEC were exposed to varying MTU doses (0–20 μM) for six hours. MTU suppresses endothelial cells' LPS-mediated hyperpermeability; its actions are most effective at concentrations greater than 5 μM. Using F-actin-labeled fluorescein phalloidin for immunofluorescence labeling of HUVEC monolayers, the impact of MTU on the actin cytoskeletal structure of the cells was investigated. F-actin was dispersed randomly throughout the control HUVEC, with actin filament bundles localized at cell borders. In HUVECs, barrier breakdown caused by LPS (100 ng/mL) showed up as the creation of paracellular gaps. Moreover, thick F-actin rings were generated and LPS-induced paracellular spaces were prevented by post-treatment with MTU (10 or 20 μM). A cell survival assay was conducted in HUVEC treated with MTU for 24 hours in order to evaluate the cytotoxicity of the drug. At doses as high as 20 μM, MTU has no effect on cell viability [1].
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| ln Vivo |
Methylthiouracil can be used to create models of brain and cardiovascular diseases in animals.
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| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Following intravenous injection of 5 mg/rat MTU, 84-90% of the dose can be recovered from the carcass within 1 minute, and 55-60% can be recovered from the carcass of animals euthanized after 3 hours. After 3 hours, the concentration of MTU in the thyroid gland is approximately 1 mg/g tissue. Antithyroid drugs can cross the placental barrier and are also detectable in breast milk. Metabolism/Metabolites 48 hours after oral administration of radioactive methylthiouracil, the metabolites excreted in rat urine are 6-methyluracil, 6-methyl-2-methylthiouracil, 6-methyl-4-oxopyrimidine, 2-amino-6-methyl-4-oxopyrimidine, and urea. |
| Toxicity/Toxicokinetics |
Interactions
Dietary iodine content was negatively correlated with the incidence of MTU-induced thyroid tumors. Topical application of 9,10-dimethyl-1,2-benzanthracene promoted the induction of cervical and vaginal sarcomas and epithelial tumors by methylthiouracil. Simultaneous administration of methylthiouracil and carbon tetrachloride prevented carbon tetrachloride-induced chronic hepatotoxicity in rats. Theophylline enhanced the effect of thyroid-stimulating hormone at the level of the thyroid adenylate cyclase system. Concomitant administration of theophylline enhanced the goitrogenic effect of 0.05% methylthiouracil. |
| References | |
| Additional Infomation |
According to California labor law, methylthiouracil may be carcinogenic. Methylthiouracil is a white crystalline powder with an onion-like odor and a bitter taste. Its saturated aqueous solution is neutral or slightly acidic. (NTP, 1992) Methylthiouracil is a pyrimidinone drug. It is a thionamide antithyroid drug that inhibits the synthesis of thyroid hormones. It is used to treat hyperthyroidism. Mechanism of Action: Thiamide derivatives (including methylthiouracil)...inhibit the synthesis and secretion of hormones until spontaneous remission occurs during the course of the disease. Therapeutic Uses: Antithyroid Drugs: Antithyroid drugs...are used to treat thyrotoxic crisis, or before or after radioactive iodine therapy. /Antithyroid Drugs/ After discontinuation, approximately 20% of patients experience a rapid relapse of hyperthyroidism within 2 months. ...Drug treatment appears to reduce the incidence of progressive eye disease. /Antithyroid Drugs/
For more complete data on the therapeutic uses of methylthiouracil (6 types), please visit the HSDB record page. Drug Warnings ...The incidence of side effects with methylthiouracil is approximately six times that of propylthiouracil. The side effects of this drug...are similar to those of propylthiouracil...The most serious side effects...include agranulocytosis, drug fever, and dermatitis. Joint pain and urticaria may occur.Cross-sensitivity reactions with other thionamide drugs may occur. ...Less common complications include...paresthesia, headache, nausea, and hair loss or depigmentation. ...Hepatitis and nephritis are very rare. /Thionamide Drugs/ ...When methylthiouracil is used to treat hyperthyroidism, nystagmus and visual illusions of motion of the surrounding environment have been reported, accompanied by severe vertigo... Methylthiouracil has been reported to affect taste and smell. /Excerpt from Table/ |
| Molecular Formula |
C5H6N2OS
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|---|---|
| Molecular Weight |
142.1789
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| Exact Mass |
142.02
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| CAS # |
56-04-2
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| PubChem CID |
667493
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| Appearance |
White to off-white solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
342.3ºC at 760 mmHg
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| Melting Point |
~330 °C (dec.)(lit.)
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| Flash Point |
160.8ºC
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| Index of Refraction |
1.638
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| LogP |
0.31
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
0
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| Heavy Atom Count |
9
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| Complexity |
197
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
HWGBHCRJGXAGEU-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C5H6N2OS/c1-3-2-4(8)7-5(9)6-3/h2H,1H3,(H2,6,7,8,9)
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| Chemical Name |
6-methyl-2-sulfanylidene-1H-pyrimidin-4-one
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 50 mg/mL (~351.67 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (17.58 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (17.58 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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