Mifepristone
Chemical Name: (11β,17β)-11-[4-(Dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)-estra-4,9-dien-3-one
Purity: ≥99%
Biological Activity
Mifepristone is a selective antagonist at progesterone (PR) and glucocorticoid (GR) receptors in vitro and in vivo. Is a silent antagonist at PR and has a higher affinity than progesterone. Has higher affinity for GR than dexamethasone (Cat. No. 1126).Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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X-ray crystal structure of the ancestral 3-ketosteroid receptor-progesterone-mifepristone complex shows mifepristone bound at the coactivator binding interface.
Colucci J, Ortlund E
PLoS ONE, 2013;8(11):e80761. -
RU 38486: a potent antiglucocorticoid in vitro and in vivo.
Gagne et al.
J.Steroid Biochem., 1985;23:247 -
Molecular mechanism of RU 486 action: a review.
Mao et al.
Mol.Cell.Biochem., 1992;109:1 -
Binding of the anti-progestin RU 486 to rat ovary steroid receptors.
Schrieber et al.
Contraception, 1983;28:77 -
Glucocorticoid receptor regulates PD-L1 and MHC-I in pancreatic cancer cells to promote immune evasion and immunotherapy resistance
Y Deng, X Xia, Y Zhao, Z Zhao, C Martinez, W Yin, J Yao, Q Hang, W Wu, J Zhang, Y Yu, W Xia, F Yao, D Zhao, Y Sun, H Ying, MC Hung, L Ma
Nature Communications, 2021;12(1):7041.
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Citations for Mifepristone
The citations listed below are publications that use Tocris products. Selected citations for Mifepristone include:
22 Citations: Showing 1 - 10
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Sex hormones alter the response of Toll-like receptor 3 to its specific ligand in fallopian tube epithelial cells.
Authors: Zandieh Et al.
Clin Exp Reprod Med 2018;45:154
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The Anti-apoptotic Effect of Ghrelin on Restraint Stress-Induced Thymus Atrophy in Mice.
Authors: Lee Et al.
Immune Network 2016;16:242
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Hierarchical glucocorticoid-endocannabinoid interplay regulates the activation of the nucleus accumbens by insulin.
Authors: Pinheiro Et al.
Brain Res.Bull. 2016;124:222
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Androgen receptor non-nuclear regulation of prostate cancer cell invasion mediated by Src and matriptase.
Authors: Zarif Et al.
Biol Reprod 2015;6:6862
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Sox2, Tlx, Gli3, and Her9 converge on Rx2 to define retinal stem cells in vivo.
Authors: Reinhardt Et al.
EMBO J 2015;34:1572
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A robust and reliable non-invasive test for stress responsivity in mice.
Authors: Zimprich Et al.
Front Behav Neurosci 2014;8:125
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Chronic stress impairs GABAergic control of amygdala through suppressing the tonic GABAA receptor currents.
Authors: Liu Et al.
Mol Brain 2014;7:32
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A transgenic zebrafish model for monitoring glucocorticoid receptor activity.
Authors: Krug Et al.
Genes Brain Behav 2014;13:478
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The role of glucocorticoid receptors in dexamethasone-induced apoptosis of neuroprogenitor cells in the hippocampus of rat pups.
Authors: Sze Et al.
World J Gastroenterol 2013;2013:628094
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Wnt activation downregulates olfactomedin-1 in Fallopian tubal epithelial cells: a microenvironment predisposed to tubal ectopic pregnancy.
Authors: Kodithuwakku Et al.
Lab Invest 2012;92:256
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Inhibition of proliferation, migration and proteolysis contribute to corticosterone-mediated inhibition of angiogenesis.
Authors: Shikatani Et al.
PLoS One 2012;7:e46625
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Stress-induced memory retrieval impairments: different time-course involvement of corticosterone and glucocorticoid receptors in dorsal and ventral hippocampus.
Authors: Dorey Et al.
Neuropsychopharmacology 2012;37:2870
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Progesterone inhibition of voltage-gated calcium channels is a potential neuroprotective mechanism against excitotoxicity.
Authors: Luoma Et al.
Steroids 2011;76:845
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Spinal synthesis of estrogen and concomitant signaling by membrane estrogen receptors regulate spinal κ- and μ-opioid receptor heterodimerization and female-specific spinal mor. antinociception.
Authors: Liu Et al.
J Neurosci 2011;31:11836
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Glucocorticoid receptors in the prefrontal cortex regulate stress-evoked DA efflux and aspects of executive function.
Authors: Butts Et al.
Proc Natl Acad Sci U S A 2011;108:18459
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Analysis of Ins sensitivity in adipose tissue of patients with primary aldosteronism.
Authors: Urbanet Et al.
J Neurophysiol 2010;95:4037
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Hepatocyte growth factor system in the mouse uterus: variation across the estrous cycle and regulation by 17-β-OE and progesterone.
Authors: Zhang
Neuroscience 2010;82:1037
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Amphetamine up-regulates activator of G-protein signaling 1 mRNA and protein levels in rat frontal cortex: the role of DA and glucocorticoid receptors.
Authors: Schwendt and McGinty
J Neurosci 2010;168:96
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Stress-induced changes in nucleus accumbens glutamate synaptic plasticity.
Authors: Campioni Et al.
Oncotarget 2009;101:3192
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Glucocorticoid receptor-mediated expression of caldesmon regulates cell migration via the reorganization of the actin cytoskeleton.
Authors: Mayanagi Et al.
J Biol Chem 2008;283:31183
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Facilitation of cardiac vagal activity by CRF-R1 antagonists during swim stress in rats.
Authors: Wood Et al.
Neuropsychopharmacology 2006;31:2580
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Behavioral stress enhances hippocampal CA1 long-term depression through the blockade of the glutamate uptake.
Authors: Yang Et al.
Mediators Inflamm 2005;25:4288
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