Chemical Name: 4-[2-Phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol
Biological ActivityPHTPP 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.
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.
Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor β antagonist activity.
Compton et al.
Compton et al.
Citations for PHTPP
The citations listed below are publications that use Tocris products. Selected citations for PHTPP include:
37 Citations: Showing 1 - 10
ERβ Accelerates Diabetic Wound Healing by Ameliorating Hyperglycemia-Induced Persistent Oxidative Stress.
Authors: Zhou Et al.
Front Endocrinol (Lausanne) 2019;10:499
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
Selective oestrogen receptor antagonists inhibit oesophageal cancer cell proliferation in vitro.
Estrogen enhances mismatch repair by induction of MLH1 expression via estrogen receptor-β.
Authors: Lu Et al.
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
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
Estrogen receptor 1 (ESR1) regulates VEGFA in adipose tissue.
Sci Rep 2017;7(1):16716
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
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
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
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
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
Mechanisms by Which 17β-OE (E2) Suppress Neuronal cox-2 Gene Expression.
Authors: Stacey Et al.
PLoS One 2016;11:e0161430
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
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
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
Oestrogen receptors interact with the α-catalytic subunit of AMP-activated protein kinase.
Authors: Lipovka Et al.
Cancer Lett 2015;35
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
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
Direct OE and diethylstilbestrol actions on early- versus late-stage prostate cancer cells.
Authors: Koong and Watson
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
Cellular mechanism of the nonmonotonic dose response of bisphenol A in rat cardiac myocytes.
Authors: Liang Et al.
Environ Health Perspect 2014;122:601
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
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
△(9)-Tetrahydrocannabinol disrupts estrogen-signaling through up-regulation of estrogen receptor β (ERβ).
Authors: Takeda Et al.
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
The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer.
Authors: Vinnedge Et al.
Front Microbiol 2012;7:e46985
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
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
Regulation of IMP3 by EGFR signaling and repression by ERβ: implications for triple-negative breast cancer.
Authors: Samanta Et al.
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
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
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
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
Bisphenol A and OE are equipotent in antagonizing cisplatin-induced cytotoxicity in breast cancer cells.
Authors: LaPensee Et al.
Progesterone inhibits estrogen-mediated neuroprotection against excitotoxicity by down-regulating estrogen receptor-β.
Authors: Aguirre Et al.
J Neurochem 2010;115:1277
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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