Mifepristone (Synonyms: RU486; RU 38486) |
رقم الكتالوجGC11637 |
الميفبريستون (RU486) هو مستقبلات هرمون البروجسترون (PR) ومضاد لمستقبلات الجلوكوكورتيكويد (GR) مع IC50s من 0.2 نانومتر و 2.6 نانومتر في الفحص المخبري
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.
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.
Average Rating: 5
(Based on Reviews and 40 reference(s) in Google Scholar.)GLPBIO products are for RESEARCH USE ONLY. Please make sure your review or question is research based.
Required fields are marked with *