| Size | Price | Stock | Qty |
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| 100mg |
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| 250mg |
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| 500mg |
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| 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 IV INJECTION OF 5 MG/RAT MTU, 84-90% OF DOSE ... RECOVERED FROM CARCASSES ... AFTER 1 MIN & 55-60% FROM CARCASSES OF ANIMALS KILLED AFTER 3 HR. AFTER 3 HR, CONCN OF MTU IN THYROID WAS APPROX 1 MG/G OF TISSUE. ANTITHYROID DRUGS CROSS THE PLACENTA & CAN ALSO BE FOUND IN MILK. /ANTITHYROID DRUGS/ Metabolism / Metabolites FORTY-EIGHT HR AFTER ORAL ADMIN OF RADIOACTIVE METHYLTHIOURACIL, METABOLITES EXCRETED IN RAT URINE WERE 6-METHYLURACIL, 6-METHYL-2-METHYLTHIOURACIL, 6-METHYL-4-OXOPYRIMIDINE, 2-AMINO-6-METHYL-4-OXOPYRIMIDINE & UREA. |
| Toxicity/Toxicokinetics |
Interactions
THERE EXISTS AN INVERSE RELATIONSHIP BETWEEN IODINE CONTENT OF DIET & MTU THYROID TUMORIGENICITY. METHYLTHIOURACIL ADMIN PROMOTED INDUCTION OF CERVICO-VAGINAL SARCOMAS & EPITHELIAL TUMORS BY LOCAL APPLICATION OF 9,10-DIMETHYL-1,2-BENZANTHRACENE. METHYLTHIOURACIL ADMIN SIMULTANEOUSLY WITH CARBON TETRACHLORIDE PREVENTED CARBON TETRACHLORIDE-INDUCED CHRONIC HEPATOTOXICITY IN RATS. THEOPHYLLINE POTENTIATES EFFECT OF THYROID STIMULATING HORMONE AT LEVEL OF THYROID ADENYL CYCLASE SYSTEM. GOITROGENIC EFFECT OF 0.05% METHYLTHIOURACIL WAS INCR BY SIMULTANEOUS ADMINISTRATION OF THEOPHYLLINE. |
| References | |
| Additional Infomation |
Methylthiouracil can cause cancer according to California Labor Code.
Methylthiouracil appears as white crystalline powder with an odor of onions and a bitter taste. A saturated aqueous solution is neutral or slightly acidic. (NTP, 1992) Methylthiouracil is a pyrimidone. A thiourea antithyroid agent that inhibits the synthesis of thyroid hormone. It is used in the treatment of hyperthyroidism. Mechanism of Action THIOAMIDE DERIVATES /WHICH INCL METHYLTHIOURACIL/ ... INHIBIT HORMONE SYNTHESIS & SECRETION UNTIL SPONTANEOUS REMISSION OCCURS DURING COURSE OF DISEASE. Therapeutic Uses Antithyroid Agents ANTITHYROID DRUGS ... ARE USED TO ... TREAT THYROTOXIC CRISIS, OR ARE GIVEN BEFORE OR AFTER RADIOACTIVE IODINE. /ANTITHYROID DRUGS/ UPON STOPPING TREATMENT, HYPERTHYROIDISM RETURNS PROMPTLY WITHIN 2 MONTHS IN ABOUT 20% OF PATIENTS. ... INCIDENCE OF PROGRESSIVE OPHTHALMOPATHY APPEARS TO BE SOMEWHAT LESS WITH DRUG THERAPY. /ANTITHYROID DRUGS/ For more Therapeutic Uses (Complete) data for METHYLTHIOURACIL (6 total), please visit the HSDB record page. Drug Warnings ... INCIDENCE OF SIDE EFFECTS FROM METHYLTHIOURACIL IS APPROX SIX TIMES HIGHER THAN THAT FOR PROPYLTHIOURACIL. SIDE EFFECTS OF DRUG ARE ... SIMILAR TO THOSE OF PROPYLTHIOURACIL ... MOST SERIOUS ... ARE GRANULAR LEUKOPENIA, DRUG FEVER, & DERMATITIS. JOINT PAINS & URTICARIA MAY OCCUR. CROSS-SENSITIVITY TO OTHER THIOURACILS MAY OCCUR. ... LESS FREQUENT COMPLICATIONS ARE ... PARESTHESIAS, HEADACHE, NAUSEA, & LOSS OR DEPIGMENTATION OF HAIR. ... HEPATITIS, & NEPHRITIS ARE VERY RARE. /THIOURACILS/ ... ADMIN OF METHYL THIOURACIL IN TREATMENT OF HYPERTHYROIDISM WAS ASSOC WITH NYSTAGMUS & VISUAL ILLUSION OF MOVEMENT OF ENVIRONMENT, ACCOMPANYING SEVERE VERTIGO ... . Methylthiouracil was reported to affect taste and smell. /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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