Home Endocrinology & Hormones Estrogen/progestogen Receptor antagonist PHTPP For research use only.

PHTPP

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

PHTPP Chemical Structure

PHTPP Chemical Structure

CAS No. 805239-56-9

Purity & Quality Control

Batch: S868601 Ethanol]84 mg/mL]false]DMSO]50 mg/mL]false]Water]Insoluble]false Purity: 99.81%
99.81

PHTPP Related Products

Signaling Pathway

Estrogen/progestogen Receptor Signaling Pathways

Estrogen/progestogen Receptor Signaling Pathway

Biological Activity

Description PHTPP is an ERβ selective antagonist with 36-fold selective for ER βover ERα.
Targets
ERβ [1]
(Cell-free)
In vitro
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].
Cell Research 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.
In Vivo
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].
Animal Research Animal Models Female B6 mice
Dosages 10 μl of 10 mM PHTPP per mouse
Administration i.p.

Chemical Information & Solubility

Molecular Weight 423.31 Formula

C20H11F6N3O
CAS No. 805239-56-9 SDF --
Smiles C1=CC=C(C=C1)C2=NN3C(=CC(=NC3=C2C4=CC=C(C=C4)O)C(F)(F)F)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

Ethanol : 84 mg/mL

DMSO : 50 mg/mL ( (118.11 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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