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  3. Mifepristone

Mifepristone (Synonyms: RU486; RU 38486)

Cat. No.: HY-13683 Purity: 98.17%
Handling Instructions

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

For research use only. We do not sell to patients.

Mifepristone Chemical Structure

Mifepristone Chemical Structure

CAS No. : 84371-65-3

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Estimated Time of Arrival: December 31
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Customer Review

Top Publications Citing Use of Products

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

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

    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.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    IC50: 0.2 nM (progesterone receptor, in T47D cells), 2.6 nM (glucocorticoid receptor, in A549 cells)[1]

    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 Cisplatin is potentiated when administered in combination with Mifepristone in HeLa cells. The IC50 of Cisplatin in combination with Mifepristone is lower (14.2 μM) than that of Cisplatin alone (34.2 μM) in HeLa cells with an approximately 2.5-fold difference. After treatment with Mifepristone, the accumulation of intracellular Cisplatin in HeLa cells is 2-fold greater, representing a significant difference (p=0.009), compare with Cisplatin alone from 0.79 to 1.52 μg/mg of protein[2].

    In Vivo

    The cervix tumor xenograft models are treated with Cisplatin 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 Cisplatin 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].

    Clinical Trial
    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 59 mg/mL (137.34 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    10 mM 0.2328 mL 1.1639 mL 2.3278 mL
    *Please refer to the solubility information to select the appropriate solvent.
    References
    Kinase Assay
    [1]

    T47D human breast cancer cells are plated in 96-well tissue culture plates at 10,000 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. Briefly, the medium is decanted and the cells are fixed for 30 min 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 1× dilution buffer, assay buffer, and 1:20 substrate/enhancer mixture are then added. After a 1-h incubation at room temperature in the dark, the lysate is transferred to a white 96-well plate and luminescence is read using a LuminoSkan Ascent[1].

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

    Cell Assay
    [2]

    The HeLa and CaSki human cervical cancer cell lines are used. The effect of Mifepristone on proliferation of cells exposed to Cisplatin 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 Cisplatin alone or the combination of Cisplatin 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. Cisplatin, 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 Cisplatin on the same schedule, and Mifepristone at the same dose 3 days previous to the administration of Cisplatin. 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.

    References
    Molecular Weight

    429.59

    Formula

    C₂₉H₃₅NO₂

    CAS No.

    84371-65-3

    SMILES

    C[[email protected]@]12[[email protected]@](C#CC)(O)CC[[email protected]@]1([H])[[email protected]]3([H])CCC4=CC(CCC4=C3[[email protected]@H](C5=CC=C(N(C)C)C=C5)C2)=O

    Shipping

    Room temperature in continental US; may vary elsewhere

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    Product Name:
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    Cat. No.:
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    Cat. No.: HY-13683