Catalog # Availability Size / Price Qty
PHTPP | CAS No. 805239-56-9 | Estrogen and Related Receptor Antagonists
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Description: Selective ERβ antagonist

Chemical Name: 4-[2-Phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol

Purity: ≥99%

Product Details
Citations (37)

Biological Activity

PHTPP is a 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

Soluble to 33 mM in DMSO and to 100 mM in ethanol
Store at RT

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. A Local Paracrine and Endocrine Network Involving TGF beta, Cox-2, ROS, and Estrogen Receptor beta Influences Reactive Stromal Cell Regulation of Prostate Cancer Cell Motility.
    Grubisha MJ, Cifuentes ME, Hammes SR, Defranco DB
    Mol. Endocrinol., 2012;26(6):940-54.
  3. 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.
  4. Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor β antagonist activity.
    Compton et al.
    J.Med.Chem., 2004;47:5872
  5. Erratum.
    Compton et al.
    J.Med.Chem., 2005;48:2724

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Citations for PHTPP

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

37 Citations: Showing 1 - 10

  1. ERβ Accelerates Diabetic Wound Healing by Ameliorating Hyperglycemia-Induced Persistent Oxidative Stress.
    Authors: Zhou Et al.
    Front Endocrinol (Lausanne)  2019;10:499
  2. Estrogen Promotes Pro-resolving Microglial Behavior and Phagocytic Cell Clearance Through the Actions of Annexin A1.
    Authors: Loiola Et al.
    Front Endocrinol (Lausanne)  2019;10:420
  3. Selective oestrogen receptor antagonists inhibit oesophageal cancer cell proliferation in vitro.
    Authors: Al-Khyatt
    BMC?Cancer  2018;18(1):121
  4. Estrogen enhances mismatch repair by induction of MLH1 expression via estrogen receptor-β.
    Authors: Lu Et al.
    Oncotarget  2017;8:38767
  5. 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
  6. 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
  7. Estrogen receptor 1 (ESR1) regulates VEGFA in adipose tissue.
    Authors: Fatima
    Sci Rep  2017;7(1):16716
  8. 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
  9. 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
  10. 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
  11. 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
  12. 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
  13. Mechanisms by Which 17β-OE (E2) Suppress Neuronal cox-2 Gene Expression.
    Authors: Stacey Et al.
    PLoS One  2016;11:e0161430
  14. 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
  15. 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
  16. 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
  17. Oestrogen receptors interact with the α-catalytic subunit of AMP-activated protein kinase.
    Authors: Lipovka Et al.
    Cancer Lett  2015;35
  18. Biologic roles of estrogen receptor-β and Ins-like growth factor-2 in triple-negative breast cancer.
    Authors: Hamilton Et al.
    Biomed Res Int  2015;2015:925703
  19. 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
  20. Direct OE and diethylstilbestrol actions on early- versus late-stage prostate cancer cells.
    Authors: Koong and Watson
    Prostate  2014;74:1589
  21. 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
  22. Cellular mechanism of the nonmonotonic dose response of bisphenol A in rat cardiac myocytes.
    Authors: Liang Et al.
    Environ Health Perspect  2014;122:601
  23. 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
  24. 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
  25. △(9)-Tetrahydrocannabinol disrupts estrogen-signaling through up-regulation of estrogen receptor β (ERβ).
    Authors: Takeda Et al.
    Oncotarget  2013;26:1073
  26. 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
  27. The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer.
    Authors: Vinnedge Et al.
    Front Microbiol  2012;7:e46985
  28. 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
  29. 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
  30. Regulation of IMP3 by EGFR signaling and repression by ERβ: implications for triple-negative breast cancer.
    Authors: Samanta Et al.
    Oncogene  2012;31:4689
  31. 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
  32. Src Inhibition with saracatinib reverses fulves. resistance in ER-positive ovarian cancer models in vitro and in vivo.
    Authors: Simpkins Et al.
    Clin Cancer Res  2012;18:5911
  33. 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
  34. 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
  35. Bisphenol A and OE are equipotent in antagonizing cisplatin-induced cytotoxicity in breast cancer cells.
    Authors: LaPensee Et al.
    Steroids  2010;290:167
  36. Progesterone inhibits estrogen-mediated neuroprotection against excitotoxicity by down-regulating estrogen receptor-β.
    Authors: Aguirre Et al.
    J Neurochem  2010;115:1277
  37. 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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