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MPP dihydrochloride

Catalog #: 1991
28 Citations 1 Review Datasheet
Catalog # Availability Size / Price Qty
1991/10
1991/50
MPP dihydrochloride | CAS No. 911295-24-4 | Estrogen and Related Receptor Antagonists
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Description: Highly selective ERα antagonist

Chemical Name: 1,3-Bis(4-hydroxyphenyl)-4-methyl-5-[4-(2-piperidinylethoxy)phenol]-1H-pyrazole dihydrochloride

Purity: ≥98%

Product Details
Citations (28)
Reviews (1)
Biological Activity Technical Data Background Product Datasheets Calculators

Biological Activity

MPP dihydrochloride is a 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:
542.5
Formula:
C29H31N3O3.2HCl
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
911295-24-4

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. The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer.
    Privette Vinnedge L, Ho S, Wikenheiser-Brokamp K, Wells S
    PLoS ONE, 2012;7(10):e46985.
  2. Molecular mechanisms underlying the rapid arrhythmogenic action of bisphenol A in female rat hearts.
    Gao X, Liang Q, Chen Y, Wang H
    Endocrinology, 2013;154(12):4607-17.
  3. 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

Product Datasheets

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Citations for MPP dihydrochloride

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

28 Citations: Showing 1 - 10

  1. Selective oestrogen receptor antagonists inhibit oesophageal cancer cell proliferation in vitro.
    Authors: Al-Khyatt
    BMC?Cancer  2018;18(1):121
  2. α-Chaconine and α-Solanine Inhibit RL95-2 Endometrium Cancer Cell Proliferation by Reducing Expression of Akt (Ser473) and ERα (Ser167).
    Authors: Arslan and Yerer
    Nutrients  2018;10
  3. Understanding the dynamics of Toll-like Receptor 5 response to flagellin and its regulation by estradiol.
    Authors: Caballero Et al.
    Sci Rep  2017;7:40981
  4. Molecular mechanisms involved in the non-monotonic effect of bisphenol-a on Ca2+ entry in mouse pancreatic β-cells.
    Authors: Villar-Pazos Et al.
    Sci Rep  2017;7:11770
  5. Estrogen receptor 1 (ESR1) regulates VEGFA in adipose tissue.
    Authors: Fatima
    Sci Rep  2017;7(1):16716
  6. Dibutyl Phthalate (DBP)-Induced Apoptosis and Neurotoxicity are Mediated via the Aryl Hydrocarbon Receptor (AhR) but not by Estrogen Receptor Alpha (ERα), Estrogen Receptor Beta (ERβ), or Peroxisome Proliferator-Activated Receptor Gamma (PPAR
    Authors: Wojtowicz Et al.
    Neurotox Res  2017;31:77
  7. 17β-OE lowers triglycerides in adipocytes via estrogen receptor α and it may be attenuated by inflammation.
    Authors: Luo Et al.
    Lipids Health Dis  2017;16:182
  8. OE Suppresses TLR4-triggered Apoptosis of Decidual Stromal Cells and Drives an Anti-inflammatory TH2 Shift by Activating SGK1.
    Authors: Lou Et al.
    Int J Biol Sci  2017;13:434
  9. Direct Regulation of Aromatase B Expression by 17β-OE and DA D1 Receptor Agonist in Adult Radial Glial Cells.
    Authors: Xing Et al.
    Cell Death Differ  2016;9:504
  10. Identification of Differential ER-Alpha Versus ER-Beta Mediated Activation of eNOS in Ovine Uterine Artery Endothelial Cells.
    Authors: Pastore Et al.
    Biol Reprod  2016;94:139
  11. 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
  12. 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
  13. Estrogen receptor subtypes mediate distinct microvascular dilation and reduction in [Ca2+]I in mesenteric microvessels of female rat.
    Authors: Mazzuca Et al.
    J Pharmacol Exp Ther  2015;352:291
  14. 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
  15. Direct OE and diethylstilbestrol actions on early- versus late-stage prostate cancer cells.
    Authors: Koong and Watson
    Prostate  2014;74:1589
  16. 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
  17. 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
  18. Gender differences in brain susceptibility to oxidative stress are mediated by levels of paraoxonase-2 expression.
    Authors: Giordano Et al.
    Free Radic Biol Med  2013;58:98
  19. Effects of 17β-OE and estrogen receptor antagonists on the proliferation of gastric cancer cell lines.
    Authors: Kim Et al.
    J Gastric Cancer  2013;13:172
  20. The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer.
    Authors: Vinnedge Et al.
    Front Microbiol  2012;7:e46985
  21. 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
  22. Estrogen-responsive nitroso-proteome in uterine artery endothelial cells: role of endothelial nitric oxide synthase and estrogen receptor-β.
    Authors: Zhang Et al.
    J Cell Physiol  2012;227:146
  23. Estrogen inhibits NPY secretion through membrane-associated estrogen receptor (ER)-α in clonal, immortalized hypothalamic neurons.
    Authors: Dhillon and Belsham
    Int J Obes (Lond)  2011;35:198
  24. 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
  25. OE selectively stimulates endothelial prostacyclin production through estrogen receptor-{alpha}.
    Authors: Sobrino Et al.
    J Mol Endocrinol  2010;44:237
  26. 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
  27. A novel OE/estrogen receptor α-dependent transcriptional mechanism controls expression of the human prolactin receptor.
    Authors: Dong Et al.
    Environ Health Perspect  2006;281:18825
  28. Estrogens protect pancreatic β-cells from apoptosis and prevent Ins-deficient diabetes mellitus in mice.
    Authors: May Et al.
    Neuropharmacology  2006;103:9232

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Effective estrogen receptor a inhibition
By Anonymous on 09/12/2024
Species: Human

To inhibit the estrogen receptor a signaling functions in M1-TAM cocultured with endothelial cells.

Effective estrogen receptor a inhibition 1991
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