PHTPP

Cat. No. 2662 37 篇引用文献提交评论说明书 / 分析证书（CoA） / 化学品安全技术说明书（SDS）

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说明： Selective ERβ antagonist

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

纯度： ≥99% (HPLC)

引用文献 (37)

通路 (1)

生物活性技术数据溶解性计算器说明书参考文献

生物活性 for PHTPP

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.

化合物库 for PHTPP

PHTPP is also offered as part of the Tocriscreen 2.0 Max. 了解 Tocris 化合物库的更多信息。

技术数据 for PHTPP

分子量	423.31
公式	C₂₀H₁₁F₆N₃O
储存	Store at RT
纯度	≥99% (HPLC)
CAS Number	805239-56-9
PubChem ID	11201035
InChI Key	AEZPAUSGTAHLOQ-UHFFFAOYSA-N
Smiles	OC1=CC=C(C=C1)C1=C2N=C(C=C(N2N=C1C1=CC=CC=C1)C(F)(F)F)C(F)(F)F

上方提供的技术数据仅供参考。批次相关数据请参见分析证书。

Tocris products are intended for laboratory research use only, unless stated otherwise.

溶解性数据 for PHTPP

	溶剂	最高浓度 mg/mL	最高浓度 mM
溶解性
	DMSO	13.96	33
	ethanol	42.33	100

制备储备液 for PHTPP

以下数据基于产品分子量 423.31。 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

浓度/溶剂体积/质量	1 mg	5 mg	10 mg
1 mM	2.36 mL	11.81 mL	23.62 mL
5 mM	0.47 mL	2.36 mL	4.72 mL
10 mM	0.24 mL	1.18 mL	2.36 mL
50 mM	0.05 mL	0.24 mL	0.47 mL

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产品说明书 for PHTPP

分析证书/产品说明书

化学品安全技术说明书

参考文献 for PHTPP

参考文献是支持产品生物活性的出版物。

Compton et al (2004) Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor β antagonist activity. J.Med.Chem. 47 5872 PMID: 15537344

Compton et al (2005) Erratum. J.Med.Chem. 48 2724

If you know of a relevant reference for PHTPP, please let us know.

按标靶查看相关产品

Estrogen and Related Receptors

关键词: PHTPP, PHTPP supplier, Selective, ERβ, ERbeta, antagonists, Estrogen, Receptors, and, Related, 2662, Tocris Bioscience

37 篇 PHTPP 的引用文献

引用文献是使用了 Tocris 产品的出版物。 PHTPP 的部分引用包括：

Pastore et al (2016) Identification of Differential ER-Alpha Versus ER-Beta Mediated Activation of eNOS in Ovine Uterine Artery Endothelial Cells. Biol Reprod 94 139 PMID: 27170438

Stacey et al (2016) Mechanisms by Which 17β-OE (E2) Suppress Neuronal cox-2 Gene Expression. PLoS One 11 e0161430 PMID: 27588681

Ma et al (2016) Estrogen replacement therapy-induced neuroprotection against brain ischemia-reperfusion injury involves the activation of astrocytes via estrogen receptor β. Sci Rep 6 21467 PMID: 26891996

Giordano et al (2013) Gender differences in brain susceptibility to oxidative stress are mediated by levels of paraoxonase-2 expression. Free Radic Biol Med 58 98 PMID: 23376469

Samanta et al (2012) Regulation of IMP3 by EGFR signaling and repression by ERβ: implications for triple-negative breast cancer. Oncogene 31 4689 PMID: 22266872

Simpkins et al (2012) Src Inhibition with saracatinib reverses fulves. resistance in ER-positive ovarian cancer models in vitro and in vivo. Clin Cancer Res 18 5911 PMID: 22896656

Al-Khyatt (2018) Selective oestrogen receptor antagonists inhibit oesophageal cancer cell proliferation in vitro. BMC Cancer 18 121 PMID: 29390981

Liang et al (2014) Cellular mechanism of the nonmonotonic dose response of bisphenol A in rat cardiac myocytes. Environ Health Perspect 122 601 PMID: 24569941

Vinnedge et al (2012) The DEK oncogene is a target of steroid hormone receptor signaling in breast cancer. Front Microbiol 7 e46985 PMID: 23071688

Zuloaga et al (2012) Estrogen receptor β dependent attenuation of cytokine-induced cyclooxygenase-2 by androgens in human brain vascular smooth muscle cells and rat mesenteric arteries. Chem Res Toxicol 77 835 PMID: 22542504

LaPensee et al (2010) Bisphenol A and OE are equipotent in antagonizing cisplatin-induced cytotoxicity in breast cancer cells. Steroids 290 167 PMID: 19796866

Bertrand et al (2015) HIV-1 Tat and cocaine mediated synaptopathy in cortical and midbrain neurons is prevented by the isoflavone Equol. Environ Health Perspect 6 894 PMID: 26441850

Gao et al (2015) 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. Biosci Rep 123 571 PMID: 25723814

Lipovka et al (2015) Oestrogen receptors interact with the α-catalytic subunit of AMP-activated protein kinase. Cancer Lett 35 PMID: 26374855

Ogo et al (2014) IGF-1 gene expression is differentially regulated by estrogen receptors α and β in mouse endometrial stromal cells and ovarian granulosa cells. J Reprod Dev 60 216 PMID: 24670778

Koong and Watson (2014) Direct OE and diethylstilbestrol actions on early- versus late-stage prostate cancer cells. Prostate 74 1589 PMID: 25213831

Gorelick et al (2014) Transgenic zebrafish reveal tissue-specific differences in estrogen signaling in response to environmental water samples. Environ Health Perspect 122 356 PMID: 24425189

Caballero et al (2017) Understanding the dynamics of Toll-like Receptor 5 response to flagellin and its regulation by estradiol. Sci Rep 7 40981 PMID: 28112187

Villar-Pazos et al (2017) Molecular mechanisms involved in the non-monotonic effect of bisphenol-a on Ca²⁺ entry in mouse pancreatic β-cells. Sci Rep 7 11770 PMID: 28924161

Harvey et al (2015) Methoxychlor and its metabolite HPTE inhibit cAMP production and expression of estrogen receptors α and β in the rat granulosa cell in vitro. Reprod Toxicol 51 72 PMID: 25549949

Hamilton et al (2015) Biologic roles of estrogen receptor-β and Ins-like growth factor-2 in triple-negative breast cancer. Biomed Res Int 2015 925703 PMID: 25874233

Takeda et al (2013) △(9)-Tetrahydrocannabinol disrupts estrogen-signaling through up-regulation of estrogen receptor β (ERβ). Oncotarget 26 1073 PMID: 23718638

Liu et al (2011) 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. J Neurosci 31 11836 PMID: 21849544

Ivanova et al (2011) Tamoxifen increases nuclear respiratory factor 1 transcription by activating estrogen receptor beta and AP-1 recruitment to adjacent promoter binding sites. FASEB J 25 1402 PMID: 21233487

Fatima (2017) Estrogen receptor 1 (ESR1) regulates VEGFA in adipose tissue. Sci Rep 7 16716 PMID: 29196658

Luo et al (2017) 17β-OE lowers triglycerides in adipocytes via estrogen receptor α and it may be attenuated by inflammation. Lipids Health Dis 16 182 PMID: 28946914

Zhou et al (2019) ERβ Accelerates Diabetic Wound Healing by Ameliorating Hyperglycemia-Induced Persistent Oxidative Stress. Front Endocrinol (Lausanne) 10 499 PMID: 31396159

Loiola et al (2019) Estrogen Promotes Pro-resolving Microglial Behavior and Phagocytic Cell Clearance Through the Actions of Annexin A1. Front Endocrinol (Lausanne) 10 420 PMID: 31297095

Wojtowicz et al (2017) 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 Neurotox Res 31 77 PMID: 27581038

Lou et al (2017) OE Suppresses TLR4-triggered Apoptosis of Decidual Stromal Cells and Drives an Anti-inflammatory TH2 Shift by Activating SGK1. Int J Biol Sci 13 434 PMID: 28529452

Lu et al (2017) Estrogen enhances mismatch repair by induction of MLH1 expression via estrogen receptor-β. Oncotarget 8 38767 PMID: 28404976

Mazzuca et al (2015) Estrogen receptor subtypes mediate distinct microvascular dilation and reduction in [Ca2+]I in mesenteric microvessels of female rat. J Pharmacol Exp Ther 352 291 PMID: 25472954

Kim et al (2013) Effects of 17β-OE and estrogen receptor antagonists on the proliferation of gastric cancer cell lines. J Gastric Cancer 13 172 PMID: 24156037

Adams et al (2012) Soy isoflavones genistein and daidzein exert anti-apoptotic actions via a selective ER-mediated mechanism in neurons following HIV-1 Tat(1-86) exposure. PLoS One 7 e37540 PMID: 22629415

Zhang et al (2012) Estrogen-responsive nitroso-proteome in uterine artery endothelial cells: role of endothelial nitric oxide synthase and estrogen receptor-β. J Cell Physiol 227 146 PMID: 21374595

Weiser et al (2009) Estrogen receptor-beta agonist diarylpropionitrile: biological activities of R- and S-enantiomers on behavior and hormonal response to stress. Endocrinology 150 1817 PMID: 19074580

Aguirre et al (2010) Progesterone inhibits estrogen-mediated neuroprotection against excitotoxicity by down-regulating estrogen receptor-β. J Neurochem 115 1277 PMID: 20977477

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Pathways for PHTPP

Estrogen Signaling Pathway

Estrogen is a steroid hormone that is responsible for the regulation of growth, differentiation and function of the reproductive system. Estrogen signaling is often dysregulated in breast cancer and osteoporosis.