PHTPP (CAS 805239-56-9): R&D Systems
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:
    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.
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
Citations:

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

18 Citations: Showing 1 - 10
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  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 2015;6:894
  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 2015;51:72
  3. Oestrogen receptors interact with the α-catalytic subunit of AMP-activated protein kinase.
    Authors: Lipovka Et al.
    Cancer Lett 2015;35
  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 2015;2015:925703
  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 2015;123:571
  6. Direct estradiol and diethylstilbestrol actions on early- versus late-stage prostate cancer cells.
    Authors: Koong and Watson
    Prostate 2014;74:1589
  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 2014;60:216
  8. 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
  9. △(9)-Tetrahydrocannabinol disrupts estrogen-signaling through up-regulation of estrogen receptor β (ERβ).
    Authors: Takeda Et al.
    Oncotarget 2013;26:1073
  10. 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
  11. The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer.
    Authors: Vinnedge Et al.
    Front Microbiol 2012;7:e46985
  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 2012;77:835
  13. Regulation of IMP3 by EGFR signaling and repression by ERβ: implications for triple-negative breast cancer.
    Authors: Samanta Et al.
    Oncogene 2012;31:4689
  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 2012;18:5911
  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.
    FASEB J 2011;25:1402
  16. Bisphenol A and estradiol are equipotent in antagonizing cisplatin-induced cytotoxicity in breast cancer cells.
    Authors: LaPensee Et al.
    Steroids 2010;290:167
  17. Progesterone inhibits estrogen-mediated neuroprotection against excitotoxicity by down-regulating estrogen receptor-β.
    Authors: Aguirre Et al.
    J Neurochem 2010;115:1277
  18. 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
Expand to show all 18 Citations

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