PHTPP

Catalog No.S8686 Batch:S868601

Technical Data

Formula

C₂₀H₁₁F₆N₃O

Molecular Weight

423.31

CAS No.

805239-56-9

Solubility (25°C)*

In vitro

Ethanol

84 mg/mL (198.43 mM)

DMSO

50 mg/mL (118.11 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution	5% DMSO 1 95% Corn oil	0.08mg/ml	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.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	0.625mg/ml	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.

* <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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description

PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.

Targets

ERβ ^[1]
(Cell-free)

In vitro

PHTPP is fully effective as an ERβ antagonist while exhibiting no significant agonism on ERα or Erβ^[1]. Treating cells with PHTPP reduces bladder cancer (BCa) cell growth and invasion, as well as MCM5 expression^[2].

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^[2].

Protocol (from reference)

Cell Assay:^{^[2]}	Cell lines HEK 293 cells Concentrations 1 μM and 10 μM Incubation Time 24 h Method 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.
Animal Study:^{^[2]}	Animal Models Female B6 mice Dosages 10 μl of 10 mM PHTPP per mouse Administration i.p.

Cell Assay:^{^[2]}

Cell lines
HEK 293 cells
Concentrations
1 μM and 10 μM
Incubation Time
24 h
Method
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.

Animal Study:^{^[2]}

Animal Models
Female B6 mice
Dosages
10 μl of 10 mM PHTPP per mouse
Administration
i.p.

References

Selleck's PHTPP has been cited by 3 publications

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

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.