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Mifepristone

Mifepristone

产品编号 T1102   CAS 84371-65-3
别名: C-1073, RU486, RU 38486, 米非司酮

Mifepristone (C-1073) 是一种黄体酮受体和糖皮质激素受体拮抗剂,在体外实验中的 IC50值分别为 0.2 nM 和 2.6 nM。

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Mifepristone Chemical Structure
Mifepristone, CAS 84371-65-3
规格 价格/CNY 货期 数量
10 mg ¥ 119 现货
25 mg ¥ 178 现货
50 mg ¥ 247 现货
100 mg ¥ 396 现货
200 mg ¥ 648 现货
500 mg ¥ 1,190 现货
1 g ¥ 1,770 现货
1 mL * 10 mM (in DMSO) ¥ 251 现货
其他形式的 Mifepristone:
产品目录号及名称: Mifepristone (T1102)
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选择批次  
纯度: 99.76%
纯度: 99.75%
纯度: 99.74%
纯度: 98.9%
纯度: 98%
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Mifepristone (C-1073) is a Progestin Antagonist. The mechanism of action of mifepristone is as a Progestational Hormone Receptor Antagonist.
靶点活性 Glucocorticoid receptor:2.6 nM, Progesterone receptor:0.2 nM
体外活性 Mifepristone按最高剂量作用于大鼠,明显减少前列腺重量,且很大程度抑制二氢睾酮引起的前列腺的生长,且诱导萎缩和细胞死亡.每天0.5 mg和1 mg Mifepristone作用于免疫抑制小鼠,可以抑制SK-OV-3肿瘤生长.
体内活性 Mifepristone抑制人类肺癌细胞A549种皮质激素诱导的糖皮质激素反应元件偶联的荧光素酶报告基因转录。而且,Mifepristone作用于人类乳腺癌细胞T47D,也阻断孕酮对碱性磷酸酶活性的诱导作用。Mifepristone抑制卵巢癌细胞SK-OV-3 和OV2008增殖,IC50分别为6.25 μM和6.91 μM。
激酶实验 Glucocorticoid receptor (GR) antagonist activity, Progesterone receptor (PR) antagonist activity: T47D alkaline phosphatase assay: T47D human breast cancer cells are plated in 96-well tissue culture plates at 104 cells per well in assay medium [RPMI medium without phenol red containing 5% (v/v) charcoal-treated FBS and 1% (v/v) penicillin–streptomycin]. Two days later, the medium is decanted and Mifepristone or control is added at a final concentration of 0.1% (v/v) dimethylsulfoxide in fresh assay medium. Twenty-four hours later, an alkaline phosphatase assay is performed using a SEAP kit. The medium is decanted and the cells are fixed for 30 minutes at room temperature with 5% (v/v) formalin. The cells are washed once at room temperature with Hanks' buffered saline solution. Equal volumes (0.05 mL) of dilution buffer, assay buffer, and 1:20 substrate/enhancer mixture are then added. After 1-hour incubation in the dark at room temperature, the lysate is transferred to a white 96-well plate and luminescence is read using a LuminoSkan Ascen. A549 reporter assay: A549 human lung carcinoma cells are washed with OPTI-MEM I. The medium is removed and lipid–DNA complex solution (1.5 μg/mL of GRE-luciferase reporter DNA in 8.5 mL OPTI-MEM I plus 6 μL/mL DMRIE-C reagent in 8.5 mL OPTI-MEM I, combined, mixed and incubated at room temperature for 40 minutes) is overlayed onto the cells in a T160 flask. The cells are incubated for 16 hours at 37 °C in a CO2 incubator. The DNA-containing medium is removed and 30 mL of growth medium containing 5% (v/v) charcoal-treated fetal bovine serum is added. After 5-6 hours, the cells are seeded in 96-well plates and incubated overnight at 37 °C. Mifepristone is then added to each well followed by dexamethasone as a corticoid challenge. The cells are incubated for 24 hours. Luciferase assay buffer is added to each well and the cells are incubated for 30 minutes at room temperature.Luciferase activity is measured in a DYNEX Microlite plate on a TopCount.
细胞实验 Cell growth is evaluated in various ovarian cancer cell lines that are subjected to dose-response or time course treatments. Media containing each of the doses of fresh steroids is replaced every 24 hours. Control groups of cells are treated with vehicle ethanol at a final concentration of less than 0.05%. Number of viable cells is evaluated by trypsinization and counting in a hemocytometer chamber using trypan blue dye exclusion. Experiments are conducted in media without phenol red and supplemented with charcoal extracted fetal bovine serum, or media containing unextracted serum and having phenol red. Similar results are obtained with both media preparations; therefore, after performing the growth curves, all subsequent experiments are conducted using media with unextracted serum and in the presence of phenol red. When indicated, the proliferation IC50s are calculated using software designed to study drug interaction. (Only for Reference)
别名 C-1073, RU486, RU 38486, 米非司酮
分子量 429.59
分子式 C29H35NO2
CAS No. 84371-65-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

DMSO: 43 mg/mL (100 mM)

Ethanol: 21.5 mg/mL (50 mM)), with gentle warming

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO / Ethanol 1 mM 2.3278 mL 11.639 mL 23.278 mL 58.195 mL
5 mM 0.4656 mL 2.3278 mL 4.6556 mL 11.639 mL
10 mM 0.2328 mL 1.1639 mL 2.3278 mL 5.8195 mL
20 mM 0.1164 mL 0.582 mL 1.1639 mL 2.9098 mL
50 mM 0.0466 mL 0.2328 mL 0.4656 mL 1.1639 mL
DMSO 100 mM 0.0233 mL 0.1164 mL 0.2328 mL 0.582 mL

计算器

摩尔浓度计算器
稀释计算器
配液计算器
分子量计算器
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输入分子式,点击计算,可计算出产品的分子量。

参考文献

1. Jiang W, et al. Bioorg Med Chem, 2006, 14(19), 6726-6732. 2. Goyeneche AA, et al. Clin Cancer Res, 2007, 13(11), 3370-3379. 3. Wang Y, et al. Stem Cells, 2012, 30(2), 169-179. 4. Cabeza M, et al. J Steroid Biochem Mol Biol, 2007, 104(3-5), 321-325.
Dydrogesterone Norethindrone Cridanimod Etonogestrel Megestrol acetate U-46619 Ulipristal acetate Estradiol dipropionate

相关化合物库

该产品包含在如下化合物库中:
抗癌药物库 抗癌临床化合物库 抗癌活性化合物库 神经退行性疾病化合物库 抗癌上市药物库 内分泌激素分子库 抗前列腺癌化合物库 经典已知活性库 抗衰老化合物库 上市药物库

剂量换算

对于不同动物的给药剂量换算,您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。

体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。

第一步:请输入动物实验的基本信息
剂量
mg/kg
每只动物体重
g
给药体积
μL
动物数量
第二步:请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
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% Tween 80
% ddH2O
计算 重置

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Mifepristone 84371-65-3 Autophagy Endocrinology/Hormones Immunology/Inflammation Others Glucocorticoid Receptor Estrogen/progestogen Receptor Progesterone Receptor NO Synthase RU38486 Inhibitor C-1073 RU-38486 NOS RU486 RU 38486 Nitric oxide synthases 米非司酮 NR3C3 inhibit C1073 RU-486 C 1073 RU 486 inhibitor

 

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