Catalog Number: 2662
Chemical Name: 4-[2-Phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol
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:
  • Formula:
  • Solubility:
    Soluble to 33 mM in DMSO and to 100 mM in ethanol
  • Purity:
  • Storage:
    Store at RT
  • 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. Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor β antagonist activity.
    Compton et al.
    J.Med.Chem., 2004;47:5872
  2. Erratum.
    Compton et al.
    J.Med.Chem., 2005;48:2724

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

Showing Results 1 - 10 of 18

  1. 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
  2. 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
  3. Oestrogen receptors interact with the α-catalytic subunit of AMP-activated protein kinase.
    Authors: Lipovka Et al.
    Cancer Lett
  4. Biologic roles of estrogen receptor-β and insulin-like growth factor-2 in triple-negative breast cancer.
    Authors: Hamilton Et al.
    Biomed Res Int
  5. 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
  6. Direct estradiol and diethylstilbestrol actions on early- versus late-stage prostate cancer cells.
    Authors: Koong and Watson
  7. 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
  8. Transgenic zebrafish reveal tissue-specific differences in estrogen signaling in response to environmental water samples.
    Authors: Gorelick Et al.
    Environ Health Perspect
  9. △(9)-Tetrahydrocannabinol disrupts estrogen-signaling through up-regulation of estrogen receptor β (ERβ).
    Authors: Takeda Et al.
  10. Effects of 17β-estradiol and estrogen receptor antagonists on the proliferation of gastric cancer cell lines.
    Authors: Kim Et al.
    J Gastric Cancer
  11. The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer.
    Authors: Vinnedge Et al.
    Front Microbiol
  12. 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
  13. Regulation of IMP3 by EGFR signaling and repression by ERβ: implications for triple-negative breast cancer.
    Authors: Samanta Et al.
  14. 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
  15. 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.
  16. Bisphenol A and estradiol are equipotent in antagonizing cisplatin-induced cytotoxicity in breast cancer cells.
    Authors: LaPensee Et al.
  17. Progesterone inhibits estrogen-mediated neuroprotection against excitotoxicity by down-regulating estrogen receptor-β.
    Authors: Aguirre Et al.
    J Neurochem
  18. Estrogen receptor-beta agonist diarylpropionitrile: biological activities of R- and S-enantiomers on behavior and hormonal response to stress.
    Authors: Weiser Et al.
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