Catalog Number: 1991
Chemical Name: 1,3-Bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride
Biological Activity
Selective, high affinity silent antagonist at ERα receptors. Displays > 200-fold selectivity for ERα over ERβ. Ki values are 2.7 and 1800 nM at ERα and ERβ receptors respectively.
Technical Data
  • M.Wt:
  • Formula:
  • Solubility:
    Soluble to 100 mM in DMSO
  • Purity:
  • Storage:
    Desiccate at +4°C
  • CAS No:
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis. All Tocris products are intended for laboratory research use only.
Background References
  1. Activities of estrogen receptor alpha- and beta-selective ligands at diverse responsive gene sites mediating transactivation or transrepression.
    Harrington et al.
    Mol.Cell.Endocrinol., 2003;206:13
  2. Antagonists selective for estrogen receptor α.
    Sun et al.
    Endocrinol., 2002;143:941

The citations listed below are publications that use Tocris products. Selected citations for MPP dihydrochloride include:

13 Citations: Showing 1 - 10
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  1. Direct Regulation of Aromatase B Expression by 17β-Estradiol and Dopamine D1 Receptor Agonist in Adult Radial Glial Cells.
    Authors: Xing Et al.
    Cell Death Differ 2016;9:504
  2. Bu-Shen-Ning-Xin decoction: inhibition of osteoclastogenesis by abrogation of the RANKL-induced NFATc1 and NF-κB signaling pathways via selective estrogen receptor α.
    Authors: Wang Et al.
    Drug Des Devel Ther 2015;9:3755
  3. HIV-1 Tat and cocaine mediated synaptopathy in cortical and midbrain neurons is prevented by the isoflavone Equol.
    Authors: Bertrand Et al.
    J Biol Chem 2015;6:894
  4. Rapid responses and mechanism of action for low-dose bisphenol S on ex vivo rat hearts and isolated myocytes: evidence of female-specific proarrhythmic effects.
    Authors: Gao Et al.
    Front Neurosci 2015;123:571
  5. Direct estradiol and diethylstilbestrol actions on early- versus late-stage prostate cancer cells.
    Authors: Koong and Watson
    Prostate 2014;74:1589
  6. Transgenic zebrafish reveal tissue-specific differences in estrogen signaling in response to environmental water samples.
    Authors: Gorelick Et al.
    Environ Health Perspect 2014;122:356
  7. High content screening of a kinase-focused library reveals compounds broadly-active against dengue viruses.
    Authors: Cruz Et al.
    PLoS Negl Trop Dis 2013;7:e2073
  8. Effects of 17β-estradiol and estrogen receptor antagonists on the proliferation of gastric cancer cell lines.
    Authors: Kim Et al.
    J Gastric Cancer 2013;13:172
  9. The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer.
    Authors: Vinnedge Et al.
    Front Microbiol 2012;7:e46985
  10. Phosphorylation of human estrogen receptor-beta at serine 105 inhibits breast cancer cell migration and invasion.
    Authors: Lam Et al.
    Mol Cell Endocrinol 2012;358:27
  11. Activation of GPR30 inhibits the growth of prostate cancer cells through sustained activation of Erk1/2, c-jun/c-fos-dependent upregulation of p21, and induction of G(2) cell-cycle arrest.
    Authors: Chan Et al.
    Proc Natl Acad Sci U S A 2010;17:1511
  12. A novel estradiol/estrogen receptor α-dependent transcriptional mechanism controls expression of the human prolactin receptor.
    Authors: Dong Et al.
    Environ Health Perspect 2006;281:18825
  13. Estrogens protect pancreatic β-cells from apoptosis and prevent insulin-deficient diabetes mellitus in mice.
    Authors: May Et al.
    Neuropharmacology 2006;103:9232
Expand to show all 13 Citations

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