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Mifepristone

Catalog #: 1479
22 Citations Datasheet / COA / SDS
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Mifepristone | CAS No. 84371-65-3 | Progesterone Receptor Antagonists
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Description: Progesterone and glucocorticoid receptor antagonist
Alternative Names: RU 486,RU 38486

Chemical Name: (11β,17β)-11-[4-(Dimethylamino)phenyl]-17-hydroxy-17-(1-propynyl)-estra-4,9-dien-3-one

Purity: ≥99%

Product Details
Citations (22)
Reviews
Biological Activity Technical Data Background Product Datasheets Calculators

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

M.Wt:
429.6
Formula:
C29H35NO2
Solubility:
Soluble to 100 mM in DMSO and to 50 mM in ethanol with gentle warming
Purity:
≥99%
Storage:
Store at RT
CAS No:
84371-65-3

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

  1. 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.
  2. RU 38486: a potent antiglucocorticoid in vitro and in vivo.
    Gagne et al.
    J.Steroid Biochem., 1985;23:247
  3. Molecular mechanism of RU 486 action: a review.
    Mao et al.
    Mol.Cell.Biochem., 1992;109:1
  4. Binding of the anti-progestin RU 486 to rat ovary steroid receptors.
    Schrieber et al.
    Contraception, 1983;28:77
  5. 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.

Product Datasheets

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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

  1. 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
  2. The Anti-apoptotic Effect of Ghrelin on Restraint Stress-Induced Thymus Atrophy in Mice.
    Authors: Lee Et al.
    Immune Network  2016;16:242
  3. Hierarchical glucocorticoid-endocannabinoid interplay regulates the activation of the nucleus accumbens by insulin.
    Authors: Pinheiro Et al.
    Brain Res.Bull.  2016;124:222
  4. Androgen receptor non-nuclear regulation of prostate cancer cell invasion mediated by Src and matriptase.
    Authors: Zarif Et al.
    Biol Reprod  2015;6:6862
  5. Sox2, Tlx, Gli3, and Her9 converge on Rx2 to define retinal stem cells in vivo.
    Authors: Reinhardt Et al.
    EMBO J  2015;34:1572
  6. A robust and reliable non-invasive test for stress responsivity in mice.
    Authors: Zimprich Et al.
    Front Behav Neurosci  2014;8:125
  7. Chronic stress impairs GABAergic control of amygdala through suppressing the tonic GABAA receptor currents.
    Authors: Liu Et al.
    Mol Brain  2014;7:32
  8. A transgenic zebrafish model for monitoring glucocorticoid receptor activity.
    Authors: Krug Et al.
    Genes Brain Behav  2014;13:478
  9. 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
  10. 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
  11. Inhibition of proliferation, migration and proteolysis contribute to corticosterone-mediated inhibition of angiogenesis.
    Authors: Shikatani Et al.
    PLoS One  2012;7:e46625
  12. 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
  13. Progesterone inhibition of voltage-gated calcium channels is a potential neuroprotective mechanism against excitotoxicity.
    Authors: Luoma Et al.
    Steroids  2011;76:845
  14. 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
  15. 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
  16. Analysis of Ins sensitivity in adipose tissue of patients with primary aldosteronism.
    Authors: Urbanet Et al.
    J Neurophysiol  2010;95:4037
  17. 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
  18. 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
  19. Stress-induced changes in nucleus accumbens glutamate synaptic plasticity.
    Authors: Campioni Et al.
    Oncotarget  2009;101:3192
  20. 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
  21. Facilitation of cardiac vagal activity by CRF-R1 antagonists during swim stress in rats.
    Authors: Wood Et al.
    Neuropsychopharmacology  2006;31:2580
  22. 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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