PHTPP

  ( 31 citations )    
Product Datasheet
Catalog Number:2662
Chemical Name:4-[2-Phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol
Product Details
Citations (31)
Reviews
Biological Activity
Selective estrogen ERβ receptor antagonist that displays 36-fold selectivity over ERα. Exhibits full antagonism at ERβ in a cotransfection assay in human endometrial cancer cells (HEC-1), with minimal effects on ERα.
Technical Data
  • M.Wt:
    423.31
  • Formula:
    C20H11F6N3O
  • Solubility:
    Soluble to 33 mM in DMSO and to 100 mM in ethanol
  • Purity:
    >99
  • Storage:
    Store at RT
  • CAS No:
    805239-56-9
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.
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Citations:

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

31 Citations: Showing 1 - 10
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  1. Selective oestrogen receptor antagonists inhibit oesophageal cancer cell proliferation in vitro.
    Authors: Al-Khyatt
    BMC?Cancer  2018;18(1):121
  2. Estrogen enhances mismatch repair by induction of MLH1 expression via estrogen receptor-β.
    Authors: Lu Et al.
    Oncotarget  2017;8:38767
  3. Estrogen receptor 1 (ESR1) regulates VEGFA in adipose tissue.
    Authors: Fatima
    Sci Rep  2017;7(1):16716
  4. 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
  5. Estradiol 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
  6. 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
  7. Estrogen replacement therapy-induced neuroprotection against brain ischemia-reperfusion injury involves the activation of astrocytes via estrogen receptor β.
    Authors: Ma Et al.
    Sci Rep  2016;6:21467
  8. Mechanisms by Which 17β-Estradiol (E2) Suppress Neuronal cox-2 Gene Expression.
    Authors: Stacey Et al.
    PLoS One  2016;11:e0161430
  9. HIV-1 Tat and cocaine mediated synaptopathy in cortical and midbrain neurons is prevented by the isoflavone Equol.
    Authors: Bertrand Et al.
    Environ Health Perspect  2015;6:894
  10. Methoxychlor and its metabolite HPTE inhibit cAMP production and expression of estrogen receptors α and β in the rat granulosa cell in vitro.
    Authors: Harvey Et al.
    Reprod Toxicol  2015;51:72
  11. 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
  12. Oestrogen receptors interact with the α-catalytic subunit of AMP-activated protein kinase.
    Authors: Lipovka Et al.
    Cancer Lett  2015;35
  13. Biologic roles of estrogen receptor-β and insulin-like growth factor-2 in triple-negative breast cancer.
    Authors: Hamilton Et al.
    Biomed Res Int  2015;2015:925703
  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.
    Biosci Rep  2015;123:571
  15. Direct estradiol and diethylstilbestrol actions on early- versus late-stage prostate cancer cells.
    Authors: Koong and Watson
    Prostate  2014;74:1589
  16. IGF-1 gene expression is differentially regulated by estrogen receptors α and β in mouse endometrial stromal cells and ovarian granulosa cells.
    Authors: Ogo Et al.
    J Reprod Dev  2014;60:216
  17. Cellular mechanism of the nonmonotonic dose response of bisphenol A in rat cardiac myocytes.
    Authors: Liang Et al.
    Environ Health Perspect  2014;122:601
  18. 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
  19. 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
  20. △(9)-Tetrahydrocannabinol disrupts estrogen-signaling through up-regulation of estrogen receptor β (ERβ).
    Authors: Takeda Et al.
    Oncotarget  2013;26:1073
  21. 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
  22. The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer.
    Authors: Vinnedge Et al.
    Front Microbiol  2012;7:e46985
  23. Soy isoflavones genistein and daidzein exert anti-apoptotic actions via a selective ER-mediated mechanism in neurons following HIV-1 Tat(1-86) exposure.
    Authors: Adams Et al.
    PLoS One  2012;7:e37540
  24. Estrogen receptor β dependent attenuation of cytokine-induced cyclooxygenase-2 by androgens in human brain vascular smooth muscle cells and rat mesenteric arteries.
    Authors: Zuloaga Et al.
    Chem Res Toxicol  2012;77:835
  25. Regulation of IMP3 by EGFR signaling and repression by ERβ: implications for triple-negative breast cancer.
    Authors: Samanta Et al.
    Oncogene  2012;31:4689
  26. 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
  27. Src Inhibition with saracatinib reverses fulvestrant resistance in ER-positive ovarian cancer models in vitro and in vivo.
    Authors: Simpkins Et al.
    Clin Cancer Res  2012;18:5911
  28. Tamoxifen increases nuclear respiratory factor 1 transcription by activating estrogen receptor beta and AP-1 recruitment to adjacent promoter binding sites.
    Authors: Ivanova Et al.
    FASEB J  2011;25:1402
  29. Bisphenol A and estradiol are equipotent in antagonizing cisplatin-induced cytotoxicity in breast cancer cells.
    Authors: LaPensee Et al.
    Steroids  2010;290:167
  30. Progesterone inhibits estrogen-mediated neuroprotection against excitotoxicity by down-regulating estrogen receptor-β.
    Authors: Aguirre Et al.
    J Neurochem  2010;115:1277
  31. Estrogen receptor-beta agonist diarylpropionitrile: biological activities of R- and S-enantiomers on behavior and hormonal response to stress.
    Authors: Weiser Et al.
    Endocrinology  2009;150:1817
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