2. Metabolic Enzyme/Protease Vitamin D Related/Nuclear Receptor Immunology/Inflammation Autophagy
  3. Endogenous Metabolite Progesterone Receptor Glucocorticoid Receptor NO Synthase Autophagy
  4. Mifepristone

Mifepristone  (Synonyms: 米非司酮; RU486; RU 38486)

目录号: HY-13683 纯度: 99.83%
COA 产品使用指南

摩尔计算器

Mifepristone (RU486) 是黄体酮受体 (PR) 和糖皮质激素受体 (GR) 拮抗剂，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 Chemical Structure

CAS No. : 84371-65-3

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥528
In-stock
50 mg ￥300
In-stock
100 mg ￥480
In-stock
500 mg ￥1550
In-stock
1 g ￥2635
In-stock
5 g   询价  
10 g   询价  

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Customer Review

Other Forms of Mifepristone:

Mifepristone 相关抗体

Top Publications Citing Use of Products

MCE 顾客使用本产品发表的 37 篇科研文献

WB
IF

    Mifepristone purchased from MCE. Usage Cited in: Chinese Pharmacological Bulletin. 2017, 33(6): 878-882.

    Effect of RU486 on elevation of intracellular calcium induced by hydrocortisone in BV-2 cellsA a: Untreated cells; b:Cells are treated with hydro; c:Cells are treated with hydro after RU486;d: Cells are treated with RU486 only.

    Mifepristone purchased from MCE. Usage Cited in: Evid Based Complement Alternat Med. 2016;2016:5850739.  [Abstract]

    The effects of XYS on the protein levels of Caveolin-1 (a) and GR (b) in PHN cells after corticosterone-induced stress injury.

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    nNOS iNOS eNOS

    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Mifepristone (RU486) is a progesterone receptor (PR) and glucocorticoid receptor (GR) antagonist with IC50s of 0.2 nM and 2.6 nM in in vitro assay[1].

    IC50 & Target

    Human Endogenous Metabolite

     

    体外研究
    (In Vitro)

    The discovery of the first competitive progesterone antagonist, Mifepristone, has stimulated an intense search for more potent and more selective antiprogestins[1]. Cell growth is evaluated after 4 days of exposure to Mifepristone at 10 μM, a concentration close to the plasma concentration achievable in humans. The antiproliferative effect of NSC 119875 is potentiated when administered in combination with Mifepristone in HeLa cells. The IC50 of NSC 119875 in combination with Mifepristone is lower (14.2 μM) than that of NSC 119875 alone (34.2 μM) in HeLa cells with an approximately 2.5-fold difference. After treatment with Mifepristone, the accumulation of intracellular NSC 119875 in HeLa cells is 2-fold greater, representing a significant difference (p=0.009), compare with NSC 119875 alone from 0.79 to 1.52 μg/mg of protein[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Mifepristone 相关抗体:
    体内研究
    (In Vivo)

    The cervix tumor xenograft models are treated with NSC 119875 alone, there is a tumor growth inhibition compare with control group. However, the tumor weight loss is even more significant (p<0.05) with the combination of NSC 119875 and Mifepristone at the doses used, showing a decrease of ~50% compared with the treatments alone by the end of the study[2]. Adult male Sprague-Dawley rats are subjected to a 4-day binge-like EtOH administration regimen (3 to 5 g/kg/i.g. every 8 hours designed to produce peak blood EtOH levels (BELs) of <300 mg/dL). Subgroups of animals receive s.c. injection of Mifepristone (20 or 40 mg/kg in peanut oil). Although Mifepristone produces no significant changes in behavior of EtOH-naïve animals, pretreatment with Mifepristone (40 mg/kg) significantly reducesthe severity of EtOH withdrawal. Asignificant interaction between diet and drug, F(5,55)=3.92, p<0.05, such that EtOH-treated animals receiving vehicle or 20 mg/kg of Mifepristone displayssignificantly more signs of EtOH withdrawal than does EtOH-naïve animals receiving the same drug treatment. Importantly, treatment with 40 mg/kg of Mifepristone significantly reduces the severity of EtOH withdrawal, in a dose-dependent manner[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Clinical Trial
    分子量

    429.59

    Formula

    C29H35NO2
    CAS 号
    性状

    固体

    颜色

    White to light yellow

    中文名称

    米非司酮；美服培酮
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验： 

    DMSO 中的溶解度 : 100 mg/mL (232.78 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.3278 mL 11.6390 mL 23.2780 mL
    5 mM 0.4656 mL 2.3278 mL 4.6556 mL
    查看完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验：

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
    ——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.82 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

      生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (5.82 mM); 澄清溶液

      此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。

      以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

      20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

    以下溶解方案，请直接配制工作液。建议现用现配，在短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比； 如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶。

    • 方案 一

      请依序添加每种溶剂： 0.5% CMC-Na/saline water

      Solubility: 10 mg/mL (23.28 mM); 悬浊液; 超声助溶

    动物溶解方案计算器
    请输入动物实验的基本信息：

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    只
    由于实验过程有损耗，建议您多配一只动物的量
    请输入您的动物体内配方组成：
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
    您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
    连续给药周期超过半月以上，请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 99.83%

    COA (290 KB) HNMR (260 KB) RP-HPLC (245 KB) MS (68 KB)

    产品使用指南 (1538 KB)
    参考文献
    Cell Assay
    [2]

    The HeLa and CaSki human cervical cancer cell lines are used. The effect of Mifepristone on proliferation of cells exposed to NSC 119875 is evaluated using the XTT assay. The assay is based on the cleavage of the yellow tetrazolium salt XTT to form an orange formazan dye by metabolically active cells. The procedure is as follows. Cells are seeded into 96-well plates; Costar at a density of 6×103 viable cells per well in 100 μL culture medium. At the end of treatment with NSC 119875 alone or the combination of NSC 119875 plus Mifepristone, 50 μL XTT is added to each well (final concentration 0.3 mg/mL), follow by incubation for 4 h in a humidified atmosphere containing 5% CO2 at 37˚C. The absorbance of the samples is measured spectrophotometrically at 492 nm using a microtiter plate ELISA reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2][3]

    Mice[2]
    Female Nude mice between 6-8 weeks of age are implanted subcutaneously with 6×106 HeLa cells in a flank. Once tumors are ~5×5 mm, the animals are pair-matched into treatment and control groups. Each group consist of 8 tumor-bearing mice. The intraperitoneal administration of drugs or vehicle begin on day 0. NSC 119875, as a single agent, is administered intraperitoneally at a dose of 3 mg/kg daily on days 1 through 3; the dose of Mifepristone, as a single agent, is 2 mg/kg/day subcutaneously for 3 days; in the combination study, the mice concurrently receive NSC 119875 on the same schedule, and Mifepristone at the same dose 3 days previous to the administration of NSC 119875. The control animals receive only the vehicle. After administration of the drugs, mice are weighed and the tumors are measured with a caliper twice weekly. The tumor weight is calculated. Experiment is conducted for 74 days, after which time all animals are weighed and humanely euthanized.
    Rats[3]
    Adult male Sprague-Dawley rats, weighing between 224 and 245 g upon arrival, are used. Mifepristone (20 or 40 mg/kg) or vehicle (peanut oil) are administered subcutaneously (s.c.) once daily following the 0800 administration of EtOH or control diet. Mifepristone is suspended in peanut oil and sonicated for 30 minutes at least 24 hours prior to injection, it is then stored at 4°C until needed. Suspension is vortexed for 10 to 15 minutes prior to and as needed throughout dosing.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    参考文献

    Mifepristone 相关分类

    完整储备液配制表

    * 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3278 mL 11.6390 mL 23.2780 mL 58.1950 mL
    5 mM 0.4656 mL 2.3278 mL 4.6556 mL 11.6390 mL
    10 mM 0.2328 mL 1.1639 mL 2.3278 mL 5.8195 mL
    15 mM 0.1552 mL 0.7759 mL 1.5519 mL 3.8797 mL
    20 mM 0.1164 mL 0.5820 mL 1.1639 mL 2.9098 mL
    25 mM 0.0931 mL 0.4656 mL 0.9311 mL 2.3278 mL
    30 mM 0.0776 mL 0.3880 mL 0.7759 mL 1.9398 mL
    40 mM 0.0582 mL 0.2910 mL 0.5820 mL 1.4549 mL
    50 mM 0.0466 mL 0.2328 mL 0.4656 mL 1.1639 mL
    60 mM 0.0388 mL 0.1940 mL 0.3880 mL 0.9699 mL
    80 mM 0.0291 mL 0.1455 mL 0.2910 mL 0.7274 mL
    100 mM 0.0233 mL 0.1164 mL 0.2328 mL 0.5820 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Mifepristone84371-65-3RU486 RU 38486米非司酮美服培酮RU 486RU-486RU38486RU 38486RU-38486Endogenous MetaboliteProgesterone ReceptorGlucocorticoid ReceptorNO SynthaseAutophagyNR3C3Nitric oxide synthasesNOSInhibitorinhibitorinhibit

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