Mifepristone (Synonyms: RU486; RU 38486) |
| カタログ番号GC11637 |
ミフェプリストン (RU486) は、プロゲステロン受容体 (PR) およびグルココルチコイド受容体 (GR) のアンタゴニストであり、in vitro アッセイで IC50 は 0.2 nM および 2.6 nM です 。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 84371-65-3
Sample solution is provided at 25 µL, 10mM.
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Mifepristone (RU486) is an orally effective progesterone (PR) receptor and glucocorticoid receptor (GR) antagonist used as an abortion drug with in vitro IC50 values of 0.2nM and 2.6nM, respectively [1]. Mifepristone is an antiprogestin that blocks the effects of progesterone, causing cervical and uterine vasodilation and uterine contractions [2]. Mifepristone can also be used to treat depression and improve neurocognitive function and mood [3].
In vitro, treatment of ovarian cancer SK-OV-3, OV2008, IGROV-1 and OV2008 cells with mifepristone (20μM) completely blocked cell growth at 24h, and the effect lasted for 3 days [4]. Treatment of human gastric adenocarcinoma MKN-45 cells with mifepristone (5, 10, 20μM) dose-dependently inhibited heterotypic adhesion of cells to matrix gel, accompanied by downregulation of integrin β3 expression in cells [5].
In vivo, oral treatment of C57BL/6 mice with mifepristone (200 mg/kg) for 1 week completely blocked the reduction in the CD4:CD8 T cell ratio in secondary lymphoid tissue (SLT) induced by enriched environment (EE)[6]. Mifepristone (25 mg/kg) treated by subcutaneous injection for 14 days in depression model rats improved interleukin 1β (IL-1β)-induced depressive-like behavior and regulated the function of microglia and astrocytes[7].
References:
[1] Jiang W, Allan G, Fiordeliso J J, et al. New progesterone receptor antagonists: phosphorus-containing 11β-aryl-substituted steroids[J]. Bioorganic & medicinal chemistry, 2006, 14(19): 6726-6732.
[2] Ashok P W, Wagaarachchi P T, Templeton A. The antiprogestogen mifepristone: a review[J]. Current Medicinal Chemistry-Immunology, Endocrine & Metabolic Agents, 2002, 2(2): 71-90.
[3] Young A H, Gallagher P, Watson S, et al. Improvements in neurocognitive function and mood following adjunctive treatment with mifepristone (RU-486) in bipolar disorder[J]. Neuropsychopharmacology, 2004, 29(8): 1538-1545.
[4] Goyeneche A A, Caron R W, Telleria C M. Mifepristone inhibits ovarian cancer cell growth in vitro and in vivo[J]. Clinical Cancer Research, 2007, 13(11): 3370-3379.
[5] Li D Q, Wang Z B, Bai J, et al. Effects of mifepristone on invasive and metastatic potential of human gastric adenocarcinoma cell line MKN-45 in vitro and in vivo[J]. World Journal of Gastroenterology: WJG, 2004, 10(12): 1726.
[6] Xiao R, Bergin S M, Huang W, et al. Environmental and genetic activation of hypothalamic BDNF modulates T-cell immunity to exert an anticancer phenotype[J]. Cancer immunology research, 2016, 4(6): 488-497.
[7] Zhang Y P, Wang H Y, Zhang C, et al. Mifepristone attenuates depression-like changes induced by chronic central administration of interleukin-1β in rats[J]. Behavioural brain research, 2018, 347: 436-445.
| Cell experiment [1]: | |
Cell lines | SK-OV-3、OV2008、IGROV-1、OV2008 cells |
Preparation Method | Subjected various ovarian cancer cell lines (SK-OV-3, Caov-3, IGROV-1, and OV2008) to a fixed, 20μM concentration of mifepristone for 3 days, with the compound being replaced every 24 h. |
Reaction Conditions | 20μM; 72h |
Applications | In all cell lines, exposure to 20μM mifepristone for 24 h was sufficient to arrest cell growth, with effects lasting for 3 days. |
| Animal experiment [2]: | |
Animal models | Male C57BL/6 mice |
Preparation Method | Mifepristone was dissolved in 0.9% NaCl, 0.25% carboxymethylcellulose, 0.2% Tween 20. Male C57BL/6 mice were housed in an enriched environment(EE) or control housing and received daily oral gavage of mifepristone (200 mg/kg body weight) or vehicle control for 1 week. |
Dosage form | 200mg/kg; p.o. |
Applications | Mifepristone completely blocked the EE-induced reduction of the CD4:CD8 T-cell ratio in the secondary lymphoid tissue (SLT). |
References: | |
| Cas No. | 84371-65-3 | SDF | |
| 同義語 | RU486; RU 38486 | ||
| Chemical Name | (8S,11R,13S,14S,17S)-11-[4-(dimethylamino)phenyl]-17-hydroxy-13-methyl-17-prop-1-ynyl-1,2,6,7,8,11,12,14,15,16-decahydrocyclopenta[a]phenanthren-3-one | ||
| Canonical SMILES | CC#CC1(CCC2C1(CC(C3=C4CCC(=O)C=C4CCC23)C5=CC=C(C=C5)N(C)C)C)O | ||
| Formula | C29H35NO2 | M.Wt | 429.59 |
| 溶解度 | ≥ 21.4795 mg/mL in DMSO, ≥ 21.45 mg/mL in EtOH with gentle warming | Storage | Store at 2-8°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 2.3278 mL | 11.639 mL | 23.278 mL |
| 5 mM | 0.4656 mL | 2.3278 mL | 4.6556 mL |
| 10 mM | 0.2328 mL | 1.1639 mL | 2.3278 mL |
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Quality Control & SDS
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- Purity: >98.00%
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Average Rating: 5 (Based on Reviews and 40 reference(s) in Google Scholar.)
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