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Methimazole Sale

(Synonyms: 甲巯咪唑) 目录号 : GC10416

An inhibitor of thyroid hormone synthesis

Methimazole Chemical Structure

Cas No.:60-56-0

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥399.00
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10g
¥557.00
现货
25g
¥1,155.00
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Sample solution is provided at 25 µL, 10mM.

产品文档

Quality Control & SDS

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实验参考方法

Cell experiment [1,2]:

Cell lines

FRTL5 thyroid cell

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.

Reacting condition

96 hrs

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]:

Animal models

Male Sprague-Dawley rats

Dosage form

Intraperitoneal administration, 300 mg/kg

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.

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.

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.

产品描述

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.

Chemical Properties

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。
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。

溶解性数据

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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
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