PHTPP

製品コードS8686 バッチS868601

印刷

化学情報

Synonyms

N/A

Storage
(From the date of receipt)

3 years -20°C powder
1 years -80°C in solvent

化学式

C₂₀H₁₁F₆N₃O

分子量

423.31

CAS No.

805239-56-9

Solubility (25°C)*

体外

Ethanol

84 mg/mL (198.43 mM)

DMSO

50 mg/mL (118.11 mM)

Water

Insoluble

体内（毎回新しく調製した物を用意してください）

Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.625mg/ml (1.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 12.5 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。	0.080mg/ml (0.19mM)	Taking the 1 mL working solution as an example, add 50 μL of 1.6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明	PHTPPは、ERαと比較してERβに36倍選択性を示すERβ選択的アンタゴニストです。
in vitro	PHTPP is fully effective as an ERβ antagonist while exhibiting no significant agonism on ERα or Erβ. Treating cells with this compound reduces bladder cancer (BCa) cell growth and invasion, as well as MCM5 expression.
in vivo	PHTPP can inhibit bladder cancer growth and invasion, resulting in better survival rate in carcinogen N-butyl-N-(4-hydroxybutyl) nitrosamine (BBN)-induced BCa mouse model.

プロトコル(参考用のみ)

細胞アッセイ	細胞株	HEK 293 cells
	濃度	1 μM and 10 μM
	反応時間	24 h
	実験の流れ	HEK 293 cells are incubated in DMEM supplemented with 10% of charcoal-stripped fetal bovine serum for 24 h and then are transfected with Erβ expressing vector (pcDNA3-ERβ), estrogen response element (ERE) firefly luciferase reporter and SV40-driven renilla expressing vector as control for 8 h followed by addition of DMSO, or 10 nM 2,3-bis(4-hydroxyphenyl)-propionitrile (DPN) with different concentrations of PHTPP. After 24 h, cells are lysed with lysis buffer and assayed.
動物実験	動物モデル	Female B6 mice
	投薬量	10 μl of 10 mM PHTPP per mouse
	投与方法	i.p.

参考

https://pubmed.ncbi.nlm.nih.gov/15537344/
https://pubmed.ncbi.nlm.nih.gov/24148819/

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Ginsenoside Rd Activates Ciliary Beat Frequency via Estrogen Receptor β and P2X7 Receptor [ Biol Pharm Bull, 2025, 48(5):657-671]	PubMed: 40399102
Different Susceptibilities of Human Melanoma Cell Lines to G2/M Blockage and Cell Death Activation in Response to the Estrogen Receptor β agonist LY500307 [ J Cancer, 2022, 13(5):1573-1587]	PubMed: 35371312
Kamishoyosan (a Japanese traditional herbal formula), which effectively reduces the aggressive biting behavior of male and female mice, and potential regulation through increase of Tph1, Tph2, and Esr2 mRNA levels [ Brain Res, 2021, 1768:147580]	PubMed: 34260963
Bisphenol A induces apoptosis through GPER-dependent activation of the ROS/Ca2+-ASK1-JNK pathway in human granulosa cell line KGN [ Ecotoxicol Environ Saf, 2020, 208:111429]	PubMed: 33039870

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。