Methylthiouracil
(Synonyms: 甲硫氧嘧啶; MTU) 目录号 : GC16007
甲基硫氧嘧啶是一种抗甲状腺药物。
Cas No.:56-04-2
Sample solution is provided at 25 µL, 10mM.
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Methylthiouracil is an antithyroid agent. Methylthiouracil suppresses the production TNF-α and IL-6, and the activation of NF-κB and ERK1/2.
HUVECs are treated with various concentrations of MTU (0-20 μM) for 6 h after the addition of LPS (100 ng/mL) for 4 h. MTU inhibits LPS-mediated hyperpermeability in endothelial cells, with the optimal effect occurring at a concentration above 5 μM. The effects of MTU are examined on HUVEC actin cytoskeletal arrangement by immunofluorescence staining of HUVEC monolayers with F-actin labeled fluorescein phalloidin. Control HUVECs exhibit a random distribution of F-actin throughout the cells, with some localization of actin filament bundles at the cell boundaries. Barrier disruption by LPS (100 ng/mL) is manifested by the formation of paracellular gaps in HUVECs. In addition, post-treatment with MTU (10 or 20 μM) results in inhibited formation of LPS-induced paracellular gaps with the formation of dense F-actin rings. To test the cytotoxicity of MTU, cellular viability assays are performed in HUVECs treated with MTU for 24 h. At concentrations up to 20 μM, MTU does not affect cell viability[1].
MTU treatment results in marked inhibition of the peritoneal leakage of dye induced by LPS. The average circulating blood volume for mice is 72 mL/kg. Because the average mouse weight in this study is 27 g, and the average blood volume is 2 mL, the injected MTU (142 or 284 μg/kg) results in a maximum concentration of 10 or 20 μM in the peripheral blood[1].
References:
[1]. Ku SK, et al. Anti-inflammatory effects of methylthiouracil in vitro and in vivo. Toxicol Appl Pharmacol. 2015 Nov 1;288(3):374-86.
Cell experiment: | MTT is used as an indicator of cell viability. Primary human umbilical vein endothelial cells (HUVECs) are grown in 96-well plates at a density of 5×103 cells/well. After 24 h, the cells are washed with fresh medium and treated with MTU (0-20 μM). After a 48 h incubation period, the cells are washed, and 100 μL of MTT (1 mg/mL) is added, followed by incubation for 4 h. Finally, DMSO (150 μL) is added to solubilize the formazan salt formed, and the amount of formazan salt is determined by measuring the OD at 540 nm using a microplate reader [1]. |
Animal experiment: | Mice[1]Male C57BL/6 mice (6-7 weeks old; average weight, 27 g) are used in this study. Mice are administered LPS (0.3 mg/mouse or 15 mg/kg, intravenously). After 4 h, the mice are intravenously treated with MTU (142 or 284 μg/kg, for 6 h) and injected with 1% Evans blue dye solution in normal saline. Six hours later, the mice are sacrificed and peritoneal exudates are collected by washing cavities with 5 mL of normal saline and by centrifuging at 200× g for 10 min. The absorbance of the supernatant is read at 650 nm. Vascular permeabilities are expressed as μg of dye/mouse that leaked into the peritoneal cavity and are determined using a standard curve. |
References: [1]. Ku SK, et al. Anti-inflammatory effects of methylthiouracil in vitro and in vivo. Toxicol Appl Pharmacol. 2015 Nov 1;288(3):374-86. | |
| Cas No. | 56-04-2 | SDF | |
| 别名 | 甲硫氧嘧啶; MTU | ||
| 化学名 | 6-methyl-2-sulfanylidene-1H-pyrimidin-4-one | ||
| Canonical SMILES | CC1=CC(=O)NC(=S)N1 | ||
| 分子式 | C5H6N2OS | 分子量 | 142.18 |
| 溶解度 | ≥ 6.65mg/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 | 7.0333 mL | 35.1667 mL | 70.3334 mL |
| 5 mM | 1.4067 mL | 7.0333 mL | 14.0667 mL |
| 10 mM | 0.7033 mL | 3.5167 mL | 7.0333 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
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- Purity: >98.00%
- COA (Certificate Of Analysis)
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