Methimazole (Synonyms: NSC 38608) |
| Catalog No.GC10416 |
El metimazol es un compuesto antitiroideo ampliamente utilizado para la investigaciÓn del hipertiroidismo.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 60-56-0
Sample solution is provided at 25 µL, 10mM.
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Methimazole (MMI) is an inhibitor of ICAM-1 (intercellular adhesion molecule-1) gene transcription via modulating the function of STAT1 (signal transducer and activator of transcription 1) [1].
ICAM-1 (intercellular adhesion molecule-1), also named as CD54, is a member of IGSF (immunoglobulin super-family adhesion molecule) which is expressed on endothelial cells and immune system cells [2]. It is encoded by ICAM-1 gene, ICAM-1 functions via binding to LFA-1 (lymphocyte function associated molecule-1) or Mac-1. It has shown that ICAM-1 abnormally expressed in patients with autoimmune thyroid diseases. Through modulating the function of STAT1 (signal transducer and activator of transcription 1), methimazole could inhibit the transcription of ICAM-1[1].
Methimazole is an inhibitor of ICAM-1 expression while H2O2 and IFN-γ both could heavily enhance the expression of ICAM-1. When tested with the modified FRTL-5 rat thyroid cells, using 500 μM methimazole pretreated the cells could inhibit the induction of ICAM-1 RNA by H2O2 and IFN-γ [1].
In tadpoles with methimazole treatment, the gene expression of thyroid hormone response was increased [3]. Through administering rats with methimazole, the CH (congenital hypothyroidism) offspring could be obtained for further research [4]. In the study, Sprague Dawley rats could be made as hypothyroid model for further research via giving 0.025% methimazole [5]. Using pregnant C57Bl/6 mice model, it was shown that methimazole could be used for mice or rat without causing gross external malformations [6].
References:
1.Kim, H., et al., Methimazole as an antioxidant and immunomodulator in thyroid cells: mechanisms involving interferon-gamma signaling and H(2)O(2) scavenging. Mol Pharmacol, 2001. 60(5): p. 972-80.
2.Kojima, R., M. Kawachi, and M. Ito, Butein suppresses ICAM-1 expression through the inhibition of IkappaBalpha and c-Jun phosphorylation in TNF-alpha- and PMA-treated HUVEC. Int Immunopharmacol, 2014. 19(14): p. 00484-6.
3.Choi, J., et al., Unliganded thyroid hormone receptor alpha regulates developmental timing via gene repression as revealed by gene disruption in Xenopus tropicalis. Endocrinology, 2014. 2.
4.O'Hare, E., et al., Effects of thyroxine treatment on histology and behavior using the methimazole model of congenital hypothyroidism in the rat. Neuroscience, 2014. 20: p. 128-138.
5.Herwig, A., et al., A thyroid hormone challenge in hypothyroid rats identifies t3 regulated genes in the hypothalamus and in models with altered energy balance and glucose homeostasis. Thyroid, 2014. 24(11): p. 1575-93.
6.Mallela, M.K., et al., Evaluation of developmental toxicity of propylthiouracil and methimazole. Birth Defects Res B Dev Reprod Toxicol, 2014. 101(4): p. 300-7.
| Cell experiment [1,2]: | |
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Cell lines |
FRTL5 thyroid cell |
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Preparation method |
The solubility of this compound in DMSO is >5.8 mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
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Reacting condition |
96 hrs |
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Applications |
Methimazole inhibited FRTL5 thyroid cell proliferation by inducing S-phase arrest of the cell cycle. Methimazole induced cell arrest in S phase. Methimazole induced a fall in the proportion of cells in both G0/G1 and G2/M phases. Treatment with methimazole caused an increase in the percentages and absolute counts of Treg lymphocytes. Treatment with methimazole significantly decreased the percentages and absolute counts of Th17 lymphocytes. |
| Animal experiment [3,4]: | |
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Animal models |
Male Sprague-Dawley rats |
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Dosage form |
Intraperitoneal administration, 300 mg/kg |
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Application |
Methimazole （300 mg/kg）induced cell death predominantly in the mature ORNs and partially reduced olfactory sensitivity in the rats. Methimazole (20-40 mg/kg) given 30 min before the nephrotoxicant reduced nephrotoxicity induced by cephaloridine, DCVC or 2-BHQ. Methimazole reduced cisplatin-induced nephrotoxicity when given 30 min before and up to 4 hr after cisplatin. Methimazole (40 mg/kg) 30 min before cephaloridine (2 g/kg) significantly protected rats against cephaloridine-induced oxidation of renal nonprotein thiols. |
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Other notes |
Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
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References: [1]. Smerdely P, Pitsiavas V, Boyages S C. Methimazole inhibits FRTL5 thyroid cell proliferation by inducing S-phase arrest of the cell cycle[J]. Endocrinology, 1993, 133(5): 2403-2406. [2]. Klatka M, Grywalska E, Partyka M, et al. Th17 and Treg cells in adolescents with Graves’ disease. Impact of treatment with methimazole on these cell subsets[J]. Autoimmunity, 2014, 47(3): 201-211. [3]. Sakamoto T, Kondo K, Kashio A, et al. Methimazole‐induced cell death in rat olfactory receptor neurons occurs via apoptosis triggered through mitochondrial cytochrome c‐mediated caspase‐3 activation pathway[J]. Journal of neuroscience research, 2007, 85(3): 548-557. [4]. Sausen P J, Elfarra A A, Cooley A J. Methimazole protection of rats against chemically induced kidney damage in vivo[J]. Journal of Pharmacology and Experimental Therapeutics, 1992, 260(1): 393-401. |
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| Cas No. | 60-56-0 | SDF | |
| Sinónimos | NSC 38608 | ||
| Chemical Name | 3-methyl-1H-imidazole-2-thione | ||
| Canonical SMILES | CN1C=CNC1=S | ||
| Formula | C4H6N2S | M.Wt | 114.17 |
| Solubility | ≥ 5.8mg/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 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 8.7589 mL | 43.7943 mL | 87.5887 mL |
| 5 mM | 1.7518 mL | 8.7589 mL | 17.5177 mL |
| 10 mM | 0.8759 mL | 4.3794 mL | 8.7589 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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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.
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 17 reference(s) in Google Scholar.)
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