Synonym
Alkiron, Antibason, Basecil, Basethyrin, Metacil, Methacil, Methylthiouracil
IUPAC/Chemical Name
4(1H)-Pyrimidinone, 2,3-dihydro-6-methyl-2-thioxo-
InChi Key
HWGBHCRJGXAGEU-UHFFFAOYSA-N
InChi Code
1S/C5H6N2OS/c1-3-2-4(8)7-5(9)6-3/h2H,1H3,(H2,6,7,8,9)
SMILES Code
c1(cc(=O)[nH]c(=S)[nH]1)C
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
Biological target:
Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
In vitro activity:
Methylthiouracil (MTU), an antithyroid drug, was examined for its effects on lipopolysaccharide (LPS)-mediated vascular inflammatory responses. Post-treatment with MTU inhibited LPS-induced barrier disruption, expression of cell adhesion molecules (CAMs), and adhesion/transendothelial migration of human neutrophils to human endothelial cells. MTU induced potent inhibition of LPS-induced endothelial cell protein C receptor (EPCR) shedding. It also suppressed LPS-induced hyperpermeability and neutrophil migration in vivo.
Reference: Toxicol Appl Pharmacol. 2015 Nov 1;288(3):374-86. https://pubmed.ncbi.nlm.nih.gov/26298005/
In vivo activity:
This study examined the effects of methylthiouracil (MTU), used as antithyroid drug, by monitoring the effects on lipopolysaccharide (LPS)- or cecal ligation and puncture (CLP)-mediated release of HMGB1, and on the modulation of HMGB1-mediated inflammatory responses. MTU also inhibited HMGB1-mediated hyperpermeability and leukocyte migration in mice. In addition, treatment with MTU reduced CLP-induced release of HMGB1 and sepsis-related mortality and pulmonary injury.
Reference: Vascul Pharmacol. 2017 Jan;88:1-10. https://pubmed.ncbi.nlm.nih.gov/26239884/
|
Solvent |
mg/mL |
mM |
comments |
| Solubility |
| DMSO |
39.0 |
274.31 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
142.18
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Jung B, Ku SK, Bae JS. Ameliorative effect of methylthiouracil on TGFBIp-induced septic responses. Biochem Biophys Res Commun. 2015 Aug 7;463(4):661-6. doi: 10.1016/j.bbrc.2015.05.120. Epub 2015 Jun 2. PMID: 26043683.
2. Ku SK, Baek MC, Bae JS. Anti-inflammatory effects of methylthiouracil in vitro and in vivo. Toxicol Appl Pharmacol. 2015 Nov 1;288(3):374-86. doi: 10.1016/j.taap.2015.08.009. Epub 2015 Aug 20. PMID: 26298005.
3. Kwak S, Ku SK, Kang H, Baek MC, Bae JS. Methylthiouracil, a new treatment option for sepsis. Vascul Pharmacol. 2017 Jan;88:1-10. doi: 10.1016/j.vph.2015.07.013. Epub 2015 Aug 1. PMID: 26239884.
4. Min G, Ku SK, Jeong S, Baek MC, Bae JS. Suppressive effects of methylthiouracil on polyphosphate-mediated vascular inflammatory responses. J Cell Mol Med. 2016 Dec;20(12):2333-2340. doi: 10.1111/jcmm.12925. Epub 2016 Jul 15. PMID: 27421058; PMCID: PMC5134378.
In vitro protocol:
1. Jung B, Ku SK, Bae JS. Ameliorative effect of methylthiouracil on TGFBIp-induced septic responses. Biochem Biophys Res Commun. 2015 Aug 7;463(4):661-6. doi: 10.1016/j.bbrc.2015.05.120. Epub 2015 Jun 2. PMID: 26043683.
2. Ku SK, Baek MC, Bae JS. Anti-inflammatory effects of methylthiouracil in vitro and in vivo. Toxicol Appl Pharmacol. 2015 Nov 1;288(3):374-86. doi: 10.1016/j.taap.2015.08.009. Epub 2015 Aug 20. PMID: 26298005.
In vivo protocol:
1. Kwak S, Ku SK, Kang H, Baek MC, Bae JS. Methylthiouracil, a new treatment option for sepsis. Vascul Pharmacol. 2017 Jan;88:1-10. doi: 10.1016/j.vph.2015.07.013. Epub 2015 Aug 1. PMID: 26239884.
2. Min G, Ku SK, Jeong S, Baek MC, Bae JS. Suppressive effects of methylthiouracil on polyphosphate-mediated vascular inflammatory responses. J Cell Mol Med. 2016 Dec;20(12):2333-2340. doi: 10.1111/jcmm.12925. Epub 2016 Jul 15. PMID: 27421058; PMCID: PMC5134378.
1: Min G, Ku SK, Jeong S, Baek MC, Bae JS. Suppressive effects of methylthiouracil on polyphosphate-mediated vascular inflammatory responses. J Cell Mol Med. 2016 Dec;20(12):2333-2340. doi: 10.1111/jcmm.12925. Epub 2016 Jul 15. PubMed PMID: 27421058; PubMed Central PMCID: PMC5134378.
2: Ku SK, Baek MC, Bae JS. Anti-inflammatory effects of methylthiouracil in vitro and in vivo. Toxicol Appl Pharmacol. 2015 Nov 1;288(3):374-86. doi: 10.1016/j.taap.2015.08.009. Epub 2015 Aug 20. PubMed PMID: 26298005.
3: Kwak S, Ku SK, Kang H, Baek MC, Bae JS. Methylthiouracil, a new treatment option for sepsis. Vascul Pharmacol. 2017 Jan;88:1-10. doi: 10.1016/j.vph.2015.07.013. Epub 2015 Aug 1. PubMed PMID: 26239884.
4: Ye ZL, Hou XX, Chen RL, Ding J, Zheng GH, Chen MZ, Tian C. Effects of methylthiouracil on the proliferation and apoptosis of rat bone marrow stromal cells. Exp Ther Med. 2014 Jun;7(6):1738-1744. Epub 2014 Mar 10. PubMed PMID: 24926377; PubMed Central PMCID: PMC4043562.
