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PHTPP

Catalog No.GC11863

estrogen ERβ receptor antagonist

Products are for research use only. Not for human use. We do not sell to patients.

PHTPP Chemical Structure

Cas No.: 805239-56-9

Size Price Stock Qty
10mg
$90.00
In stock
50mg
$351.00
In stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Protocol

Cell experiment:

Cells are plated at a density of 3 to 4×105 in 1 mL of medium per well in a 24-well plate for cell viability and cAMP analysis. Cells are cultured in Dulbecco’s Modified Eagle Medium with PHTPP (1 μM), or ethanol (0.1%) as the vehicle. The incubator is set to an atmosphere of 5% CO2 in air at 37°C, and cultures are allowed to acclimate for at least 24 h. The culture medium is then aspirated and replaced with serum-free DMEM/F12 containing 0.1 μM androstenedione. The cells are collected for intracellular cAMP and to test cell viability[1].

References:

[1]. Compton DR, et al. Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor beta antagonist activity. J Med Chem. 2004 Nov 18;47(24):5872-93.
[2]. Ogo Y, et al. 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. Epub 2014 Mar 25.

Background

PHTPP is a selective ERβ antagonist.

PHTPP is a selective ERβ antagonist. PHTPP reduces FSH-mediated cAMP production by 80% (pIgf1 mRNA expression, and facilitates the DPN-induced increase in class 1 Igf1 mRNA expression[2].

References:
[1]. Compton DR, et al. Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor beta antagonist activity. J Med Chem. 2004 Nov 18;47(24):5872-93.
[2]. Ogo Y, et al. 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. Epub 2014 Mar 25.

Chemical Properties

Cas No. 805239-56-9 SDF
Chemical Name 4-(2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl)phenol
Canonical SMILES FC(F)(C1=CC(C(F)(F)F)=NC2=C(C(C=C3)=CC=C3O)C(C4=CC=CC=C4)=NN21)F
Formula C20H11F6N3O M.Wt 423.31
Solubility ≤30mg/ml in ethanol;50mg/ml in DMSO Storage Store at RT
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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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
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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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.

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Average Rating: 5 ★★★★★ (Based on Reviews and 23 reference(s) in Google Scholar.)

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