Methimazole
(Synonyms: 甲巯咪唑) 目录号 : GC10416
An inhibitor of thyroid hormone synthesis
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 | |
| 别名 | 甲巯咪唑 | ||
| 化学名 | 3-methyl-1H-imidazole-2-thione | ||
| Canonical SMILES | CN1C=CNC1=S | ||
| 分子式 | C4H6N2S | 分子量 | 114.17 |
| 溶解度 | ≥ 5.8mg/mL in DMSO | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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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 |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet