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Submit ReviewMifepristone
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% (HPLC)
Biological Activity for Mifepristone
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).
Compound Libraries for Mifepristone
Mifepristone is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
Technical Data for Mifepristone
| M. Wt | 429.6 |
| Formula | C29H35NO2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 84371-65-3 |
| PubChem ID | 55245 |
| InChI Key | VKHAHZOOUSRJNA-GCNJZUOMSA-N |
| Smiles | [H][C@@]23CCC1=CC(CCC1=C2[C@@H]([C@]5=CC=C(N(C)C)C=C5)C[C@@]4(C)[C@]([H])3CC[C@@](C#CC)4O)=O |
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.
Solubility Data for Mifepristone
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 42.96 | 100 | |
| ethanol | 21.48 | 50 with gentle warming |
Preparing Stock Solutions for Mifepristone
The following data is based on the product molecular weight 429.6. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.33 mL | 11.64 mL | 23.28 mL |
| 5 mM | 0.47 mL | 2.33 mL | 4.66 mL |
| 10 mM | 0.23 mL | 1.16 mL | 2.33 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.47 mL |
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Product Datasheets for Mifepristone
References for Mifepristone
References are publications that support the biological activity of the product.
Gagne et al (1985) RU 38486: a potent antiglucocorticoid in vitro and in vivo. J.Steroid Biochem. 23 247 PMID: 2864478
Mao et al (1992) Molecular mechanism of RU 486 action: a review. Mol.Cell.Biochem. 109 1 PMID: 1614417
Schrieber et al (1983) Binding of the anti-progestin RU 486 to rat ovary steroid receptors. Contraception 28 77 PMID: 6627946
If you know of a relevant reference for Mifepristone, please let us know.
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Keywords: Mifepristone, Mifepristone supplier, Glucocorticoid, progesterone, antagonists, glucocorticoid, Receptors, RU486, RU38486, RU, 486, 38486, Progesterone, Receptor, 1479, Tocris Bioscience
22 Citations for Mifepristone
Citations are publications that use Tocris products. Selected citations for Mifepristone include:
Reinhardt et al (2015) Sox2, Tlx, Gli3, and Her9 converge on Rx2 to define retinal stem cells in vivo. EMBO J 34 1572 PMID: 25908840
Sze et al (2013) The role of glucocorticoid receptors in dexamethasone-induced apoptosis of neuroprogenitor cells in the hippocampus of rat pups. World J Gastroenterol 2013 628094 PMID: 23401645
Luoma et al (2011) Progesterone inhibition of voltage-gated calcium channels is a potential neuroprotective mechanism against excitotoxicity. Steroids 76 845 PMID: 21371490
Butts et al (2011) Glucocorticoid receptors in the prefrontal cortex regulate stress-evoked DA efflux and aspects of executive function. Proc Natl Acad Sci U S A 108 18459 PMID: 22032926
Mayanagi et al (2008) Glucocorticoid receptor-mediated expression of caldesmon regulates cell migration via the reorganization of the actin cytoskeleton. J Biol Chem 283 31183 PMID: 18772142
Campioni et al (2009) Stress-induced changes in nucleus accumbens glutamate synaptic plasticity. Oncotarget 101 3192 PMID: 19357347
Zandieh et al (2018) Sex hormones alter the response of Toll-like receptor 3 to its specific ligand in fallopian tube epithelial cells. Clin Exp Reprod Med 45 154 PMID: 30538945
Liu et al (2011) 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. J Neurosci 31 11836 PMID: 21849544
Kodithuwakku et al (2012) Wnt activation downregulates olfactomedin-1 in Fallopian tubal epithelial cells: a microenvironment predisposed to tubal ectopic pregnancy. Lab Invest 92 256 PMID: 21968811
Shikatani et al (2012) Inhibition of proliferation, migration and proteolysis contribute to corticosterone-mediated inhibition of angiogenesis. PLoS One 7 e46625 PMID: 23056375
Dorey et al (2012) Stress-induced memory retrieval impairments: different time-course involvement of corticosterone and glucocorticoid receptors in dorsal and ventral hippocampus. Neuropsychopharmacology 37 2870 PMID: 22948976
Zhang (2010) Hepatocyte growth factor system in the mouse uterus: variation across the estrous cycle and regulation by 17-β-OE and progesterone. Neuroscience 82 1037 PMID: 20147731
Schwendt and McGinty (2010) Amphetamine up-regulates activator of G-protein signaling 1 mRNA and protein levels in rat frontal cortex: the role of DA and glucocorticoid receptors. J Neurosci 168 96 PMID: 20298760
Yang et al (2005) Behavioral stress enhances hippocampal CA1 long-term depression through the blockade of the glutamate uptake. Mediators Inflamm 25 4288 PMID: 15858055
Lee et al (2016) The Anti-apoptotic Effect of Ghrelin on Restraint Stress-Induced Thymus Atrophy in Mice. Immune Network 16 242 PMID: 27574503
Zarif et al (2015) Androgen receptor non-nuclear regulation of prostate cancer cell invasion mediated by Src and matriptase. Biol Reprod 6 6862 PMID: 25730905
Krug et al (2014) A transgenic zebrafish model for monitoring glucocorticoid receptor activity. Genes Brain Behav 13 478 PMID: 24679220
Zimprich et al (2014) A robust and reliable non-invasive test for stress responsivity in mice. Front Behav Neurosci 8 125 PMID: 24782732
Wood et al (2006) Facilitation of cardiac vagal activity by CRF-R1 antagonists during swim stress in rats. Neuropsychopharmacology 31 2580 PMID: 16710322
Pinheiro et al (2016) Hierarchical glucocorticoid-endocannabinoid interplay regulates the activation of the nucleus accumbens by insulin. Brain Res.Bull. 124 222 PMID: 27208730
Urbanet et al (2010) Analysis of Ins sensitivity in adipose tissue of patients with primary aldosteronism. J Neurophysiol 95 4037 PMID: 20484481
Liu et al (2014) Chronic stress impairs GABAergic control of amygdala through suppressing the tonic GABAA receptor currents. Mol Brain 7 32 PMID: 24758222
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