Methimazole是一种抗甲状腺药物，具有抗炎活性，抑制prostaglandin H synthase的IC50值为10µM。
Cas No.:60-56-0
Sample solution is provided at 25 µL, 10mM.
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Methimazole is an antithyroid agent and has anti-inflammatory activity, with an IC50 value of 10µM for inhibiting prostaglandin H synthase [1]. Methimazole prevents oxidation and tyrosine coupling of iodide absorbed into the thyroid gland, which in turn inhibits thyroxine synthesis [2]. Methimazole has been widely used to regulate the mitochondrial function of liver cells and to reduce the level of glutathione[3].
In vitro, Methimazole treatment (40mM) for 48 hours significantly inhibited the viability of PANC-1 cells and increased the production of reactive oxygen species (ROS)[4]. Treatment with 2mM Methimazole for 24 hours significantly caused S-phase arrest in FRTL5 thyroid cells[5]. Treatment with 10mM Methimazole for 3 days significantly increased the sensitivity of thyroid epithelial cells (TECs) to H2O2, promoted cell apoptosis, and caused irregular shapes of the cell nuclei[6].
In vivo, Methimazole treatment via a single intraperitoneal injection at a dose of 400mg/kg for 5 hours significantly induced a decrease in the liver mitochondrial membrane potential of the mice, and reduced the contents of ATP and glutathione in the liver mitochondria[7]. Administering 60mg/kg of Methimazole orally daily for 4 weeks resulted in a decrease in rectal temperature and body weight in Wistar rats and caused cell damage in the liver, kidneys, spleen, and heart[8].
References:
[1] Lagorce J F, Moulard T, Rousseau A, et al. Anti-inflammatory action of methimazole[J]. Pharmacology, 1997, 55(4): 173-178.
[2] Liu Y, Li Q, Xu Y, et al. Comparison of the safety between propylthiouracil and methimazole with hyperthyroidism in pregnancy: A systematic review and meta-analysis[J]. PLoS One, 2023, 18(5): e0286097.
[3] Heidari R, Babaei H, Eghbal M. Mechanisms of methimazole cytotoxicity in isolated rat hepatocytes[J]. Drug and chemical toxicology, 2013, 36(4): 403-411.
[4] Yazıcı Ö, Kara M, Boran T, et al. The role of endoplasmic reticulum stress in cell injury induced by methimazole on pancreatic cells[J]. Advanced pharmaceutical bulletin, 2022, 13(1): 196.
[5] 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.
[6] Landex N L, Thomsen J, Kayser L. Methimazole increases H2O2 toxicity in human thyroid epithelial cells[J]. Acta histochemica, 2006, 108(6): 431-439.
[7] Niknahad H, Jamshidzadeh A, Heidari R, et al. Paradoxical effect of methimazole on liver mitochondria: in vitro and in vivo[J]. Toxicology letters, 2016, 259: 108-115.
[8] Cano-Europa E, Blas-Valdivia V, Franco-Colin M, et al. Methimazole-induced hypothyroidism causes cellular damage in the spleen, heart, liver, lung and kidney[J]. Acta histochemica, 2011, 113(1): 1-5.
Methimazole是一种抗甲状腺药物，具有抗炎活性，抑制prostaglandin H synthase的IC50值为10µM[1]。Methimazole可防止被甲状腺摄取的碘发生氧化和酪氨酸偶联，从而抑制甲状腺素的合成[2]。Methimazole已被广泛用于调节肝细胞的线粒体功能并降低谷胱甘肽水平[3]。
在体外，40mM的Methimazole处理PANC-1细胞48小时，显著抑制了细胞活力，并增加了活性氧(ROS)的产生[4]。2mM的Methimazole处理FRTL5甲状腺细胞24小时，显著引起了S期阻滞[5]。10mM的Methimazole处理3天，显著增加了甲状腺上皮细胞(TECs)对H2O2的敏感性，促进了细胞凋亡，并导致了细胞核形态不规则[6]。
在体内，单次腹腔注射400mg/kg剂量的Methimazole，处理5小时，显著诱导了小鼠肝脏线粒体膜电位的下降，并降低了肝脏线粒体中ATP和谷胱甘肽的含量[7]。每日口服60mg/kg的Methimazole，连续4周，导致Wistar大鼠的直肠温度和体重下降，并引起肝脏、肾脏、脾脏和心脏的细胞损伤[8]。
| Cell experiment [1]: | |
Cell lines | PANC-1 cells |
Preparation Method | PANC-1 cells were grown in Dulbecco's Modified Eagle Medium (DMEM) with 10% (v/v) fetal bovine serum (FBS), 100μg/ml streptomycin, and 100U/ml penicillin at 37°C in 5% CO2/atmosphere. PANC-1 cells (1×104) were seeded into each well of a 96-well plate for 24h. For cytotoxicity assessment, different concentrations of Methimazole (0, 10, 20, 40, 100, and 200mM) were used for 48h exposure. The medium was used for control. After 48 hours exposure, the cell viability was analyzed. |
Reaction Conditions | 0, 10, 20, 40, 100, and 200mM; 48h |
Applications | Methimazole treatment significantly decreased the cell viability of PANC-1 cells in a dose-dependent manner. |
| Animal experiment [2]: | |
Animal models | Male Wistar rats |
Preparation Method | Male Wistar rats were housed singly in 20cm×30cm×18cm metal cages with food and water ad libitum. The cages were located together in racks (to maintain auditory and olfactory contact) in a light (08:00-20:00 light on) and temperature (21±1°C) controlled room. The rats were allowed to acclimatize to the colony-room conditions for at least 1 week before starting the experiments. Rats received 60mg/kg/day of Methimazole in drinking water daily for 4 weeks. The spleen, heart, liver, lung, and kidney of rats were removed for analysis. |
Dosage form | 60mg/kg/day for 4 weeks; p.o. |
Applications | Methimazole treatment significantly caused cellular damage in the liver, kidneys, spleen, and heart in rats. |
References: | |
| 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 |
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| 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 | 875.9 μL | 4.3794 mL | 8.7589 mL |
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| 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 |
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| % 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，
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2.
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