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.
|Storage||Desiccate at +4°C|
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.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 542.5. Batch specific molecular weights may vary from batch to batch due to solvent 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||1.84 mL||9.22 mL||18.43 mL|
|5 mM||0.37 mL||1.84 mL||3.69 mL|
|10 mM||0.18 mL||0.92 mL||1.84 mL|
|50 mM||0.04 mL||0.18 mL||0.37 mL|
References are publications that support the products' biological activity.
Harrington et al (2003) Activities of estrogen receptor alpha- and beta-selective ligands at diverse responsive gene sites mediating transactivation or transrepression. Mol.Cell.Endocrinol. 206 13 PMID: 12943986
If you know of a relevant reference for MPP dihydrochloride, please let us know.
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Keywords: MPP dihydrochloride, supplier, selective, Erα, receptor, antagonist;, ERalpha, antagonists, ER, ERR, Estrogen, Receptors, Estrogen, and, Related, Receptors, Estrogen, and, Related, Receptors, Tocris Bioscience
14 Citations for MPP dihydrochloride
Citations are publications that use Tocris products. Selected citations for MPP dihydrochloride include:
Vinnedge et al (2012) The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer. Front Microbiol 7 e46985 PMID: 23071688
Fatima (2017) Estrogen receptor 1 (ESR1) regulates VEGFA in adipose tissue. Sci Rep 7 16716 PMID: 29196658
Xing et al (2016) Direct Regulation of Aromatase B Expression by 17β-Estradiol and Dopamine D1 Receptor Agonist in Adult Radial Glial Cells. Cell Death Differ 9 504 PMID: 26793050
Wang et al (2015) 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. Drug Des Devel Ther 9 3755 PMID: 26229438
Gao et al (2015) 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. Front Neurosci 123 571 PMID: 25723814
Bertrand et al (2015) HIV-1 Tat and cocaine mediated synaptopathy in cortical and midbrain neurons is prevented by the isoflavone Equol. J Biol Chem 6 894 PMID: 26441850
Lam et al (2012) Phosphorylation of human estrogen receptor-beta at serine 105 inhibits breast cancer cell migration and invasion. Mol Cell Endocrinol 358 27 PMID: 22370157
Chan et al (2010) 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. Proc Natl Acad Sci U S A 17 1511 PMID: 20203690
Koong and Watson (2014) Direct estradiol and diethylstilbestrol actions on early- versus late-stage prostate cancer cells. Prostate 74 1589 PMID: 25213831
Gorelick et al (2014) Transgenic zebrafish reveal tissue-specific differences in estrogen signaling in response to environmental water samples. Environ Health Perspect 122 356 PMID: 24425189
Cruz et al (2013) High content screening of a kinase-focused library reveals compounds broadly-active against dengue viruses. PLoS Negl Trop Dis 7 e2073 PMID: 23437413
Kim et al (2013) Effects of 17β-estradiol and estrogen receptor antagonists on the proliferation of gastric cancer cell lines. J Gastric Cancer 13 172 PMID: 24156037
May et al (2006) Estrogens protect pancreatic β-cells from apoptosis and prevent insulin-deficient diabetes mellitus in mice. Neuropharmacology 103 9232 PMID: 16754860
Dong et al (2006) A novel estradiol/estrogen receptor α-dependent transcriptional mechanism controls expression of the human prolactin receptor. Environ Health Perspect 281 18825 PMID: 16651265
Do you know of a great paper that uses MPP dihydrochloride from Tocris? If so please let us know.
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