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CAS No.: 805239-56-9

PHTPP Catalog No. CSN19690

Synonyms: PHTPP

PHTPP has selective antagonism of estrogen ERβ receptor .

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靶点选择性

生物活性

实验方案

技术信息

生物活性

描述ER (Estrogen Receptor) is the receptor of estrogens. The steroid hormones and their receptors are involved in the regulation of eukaryotic gene expression and affect cellular proliferation and differentiation in target tissues. ER has two receptor subtypes, ERα and ERβ. ERα and ERβ have different tissue distributions and each receptor has similar or unique roles in estrogen-dependent gene expressions. PHTPP is an selective ERβ antagonist. PHTPP showed a relative binding affinity 36-fold selective for ERβ than ERα^[1]. In HEC-1-A cells transfected with estrogen-responsive reporter gene plasmids, 1 μM PHTPP inhibited estrogen stimulated ERβ activity but did not suppress estrogen stimulated ERα activity^[2]. 10 μM PHTPP effectively inhibited ERβ transcriptional activity in HEK293 cells transfected with ERβ expressing vector^[3]. At the concentrations of 10, 15 and 20 μM, PHTPP dose-dependently inhibited the growth of bladder cancer cells J82, 647v and T24 detected at day 6. J82 cells treated by 20 μM PHTPP had less invasive ability than control group^[3]. In a mouse model of BBN-induced bladder cancer, 10 μl of 10 mM PHTPP solution i.p. injected every other day for 12 weeks resulted in smaller tumor masses and better survival rate compared to control group. Moreover, 100% of the mice in the control group developed tumors with muscle invasion while the data was only around 33% in the PHTPP treated group^[3].
参考文献

[1] Compton DR, Sheng S, Carlson KE, Rebacz NA, Lee IY, Katzenellenbogen BS, Katzenellenbogen JA. Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor beta antagonist activity. J Med Chem. 2004 Nov 18;47(24):5872-93. doi: 10.1021/jm049631k. Erratum in: J Med Chem. 2005 Apr 7;48(7):2724. PMID: 15537344.
[2] Ogo Y, Taniuchi S, Ojima F, Hayashi S, Murakami I, Saito Y, Takeuchi S, Kudo T, Takahashi S. 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. 2014;60(3):216-23. doi: 10.1262/jrd.2013-085. Epub 2014 Mar 25. PMID: 24670778; PMCID: PMC4085386.
[3] Hsu I, Chuang KL, Slavin S, Da J, Lim WX, Pang ST, O'Brien JH, Yeh S. Suppression of ERβ signaling via ERβ knockout or antagonist protects against bladder cancer development. Carcinogenesis. 2014 Mar;35(3):651-61. doi: 10.1093/carcin/bgt348. Epub 2013 Oct 22. PMID: 24148819.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.3623 mL
- 11.8117 mL
- 23.6233 mL
- 5 mM
- 0.4725 mL
- 2.3623 mL
- 4.7247 mL
- 10 mM
- 0.2362 mL
- 1.1812 mL
- 2.3623 mL

技术信息

CAS号

805239-56-9

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H11F6N3O

运输

蓝冰

分子量

423.31

别名

PHTPP

溶解度

DMSO	80.0 mg/mL (189.0 mM) warming
Water	insoluble

动物实验配方

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