2. Vitamin D Related/Nuclear Receptor
  3. Estrogen Receptor/ERR
  4. PHTPP

PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα.

For research use only. We do not sell to patients.

CAS No. : 805239-56-9

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Customer Review

Based on 30 publication(s) in Google Scholar

Other Forms of PHTPP:

PHTPP Related Antibodies

Top Publications Citing Use of Products

30 Publications Citing Use of MCE PHTPP

Cell Imaging/Staining
Flow Cytometry
WB

    PHTPP purchased from MedChemExpress. Usage Cited in: Cell Mol Biol Lett. 2025 Nov 13;30(1):136.  [Abstract]

    Using selective antagonists of ERβ (PHTPP) and ERα (AZD9496), it was confirmed that the mechanism by which E0703 improves cell viability is mediated by ERβ.

    PHTPP purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2024 Mar 25;20(6):2236-2260.

    Meg-01 cells were analyzed by flow cytometry after treatment with genistein (20 μM), PHTPP (20 μM), and a combination of the two.

    PHTPP purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2024 Mar 25;20(6):2236-2260.

    The expression levels of ERβ/GAPDH, p-PI3K/PI3K, p-ERK/ERK, and NF-E2/GAPDH were detected by western blot after Meg-01 cells were treated with genistin (20 μM), PHTPP (20 μM) or both intervention for 5 days.

    PHTPP purchased from MedChemExpress. Usage Cited in: Int J Biol Sci. 2024 Mar 25;20(6):2236-2260.

    PHTPP (1 μM). The expression level of ERβ protein in TCMK-1 cells after PHTPP treatment was detected by Western blotting.

    PHTPP purchased from MedChemExpress. Usage Cited in: Phytomedicine. 2024 Jan:123:155218.  [Abstract]

    PHTPP (1 μM). ROS levels and apoptosis in TCMK-1 cells after ERβ gene overexpression.

    View All Estrogen Receptor/ERR Isoform Specific Products:

    View All Isoforms
    Estrogen receptor ERα ERβ ERRα ERRβ ERRγ

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    PHTPP is a selective estrogen receptor β (ERβ) antagonist with 36-fold selectivity over ERα[1].

    IC50 & Target

    ERβ[1]
    In Vitro

    PHTPP is a selective ERβ antagonist. PHTPP reduces FSH-mediated cAMP production by 80% (p<0.01) while it has no effect on basal cAMP[1]. PHTPP (10-6 M) inhibits E2-stimulated ERβ activity, but does not suppress E2-stimulated ERα activity. A high dose of PHTPP (10-6 M) slightly increases class 1 Igf1 mRNA expression, and facilitates the DPN-induced increase in class 1 Igf1 mRNA expression[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    PHTPP Related Antibodies
    Molecular Weight

    423.31

    Formula

    C20H11F6N3O
    CAS No.
    Appearance

    Solid

    Color

    Light yellow to yellow

    SMILES

    OC1=CC=C(C2=C3N=C(C(F)(F)F)C=C(C(F)(F)F)N3N=C2C4=CC=CC=C4)C=C1
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 15.38 mg/mL (36.33 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

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    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (5.91 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    • Protocol 2

      Add each solvent one by one:  10% DMSO    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.91 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

    For the following dissolution methods, please prepare the working solution directly. It is recommended to prepare fresh solutions and use them promptly within a short period of time.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  15% Cremophor EL    85% Saline

      Solubility: 5 mg/mL (11.81 mM); Suspended solution; Need ultrasonic

    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation
    References
    Cell Assay
    [1]

    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].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.3623 mL 11.8117 mL 23.6233 mL 59.0584 mL
    5 mM 0.4725 mL 2.3623 mL 4.7247 mL 11.8117 mL
    10 mM 0.2362 mL 1.1812 mL 2.3623 mL 5.9058 mL
    15 mM 0.1575 mL 0.7874 mL 1.5749 mL 3.9372 mL
    20 mM 0.1181 mL 0.5906 mL 1.1812 mL 2.9529 mL
    25 mM 0.0945 mL 0.4725 mL 0.9449 mL 2.3623 mL
    30 mM 0.0787 mL 0.3937 mL 0.7874 mL 1.9686 mL
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    PHTPP Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    PHTPP805239-56-9Estrogen Receptor/ERRInhibitorinhibitorinhibit

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