Art. -Nr.: HY-103456

PHTPP

Name: PHTPP
Brand: MedChemExpress
SKU: HY-103456
Price: 60.00 USD
Availability: InStock
Rating: 5 (34 reviews)

34 Cited Publications

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Based on 34 publication(s) in Google Scholar

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

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Reinheit : 99.56%
CAS. Nr.: 805239-56-9
Formel: C₂₀H₁₁F₆N₃O
Molecular Weight:423.31

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

PHTPP Chemical Structure

CAS. Nr.: 805239-56-9

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
Chemical Information
Publications (34)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Protokoll (1)
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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

IC₅₀ & Target

ERβ^[1]

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen :

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. Further protocols information, click here.

Chemical Information

CAS. Nr. 805239-56-9
Appearance Solid
Molecular Weight 423.31
Formel C₂₀H₁₁F₆N₃O
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
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (34)

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Journal Impact Factor

Cell Mol Biol Lett

E0703 targets ERβ to facilitate the upregulation of GLI3, thereby alleviating irradiation-induced DNA damage on lymphocytes. [Abstract]

2025 Nov 13;30(1):136. PMID: 41233737

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.
Int J Biol Sci

Genistin: A Novel Estrogen Analogue Targeting ERβ to Alleviate Thrombocytopenia. [Abstract]

2024 Mar 25;20(6):2236-2260. PMID: 38617546

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

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. [Abstract]

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. [Abstract]

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

Genistein ameliorates lupus nephritis via enhancing ERβ-mediated inhibition of STAT3-driven inflammation. [Abstract]

2026 Apr:153:157917. PMID: 41653614
Phytomedicine

Effects and mechanisms of frehmaglutin D and rehmaionoside C improve LPS-induced acute kidney injury through the estrogen receptor-mediated TLR4 pathway in vivo and in vitro. [Abstract]

2024 Jan:123:155218. PMID: 37980806

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.
Phytomedicine

miR-363-3p/PTEN is involved in the regulation of lipid metabolism by genistein in HepG2 cells via ERβ. [Abstract]

2023 Jul:115:154839. PMID: 37121060
Phytomedicine

Silibinin improves L-cell mass and function through an estrogen receptor-mediated antioxidative mechanism. [Abstract]

2022 May:99:154022. PMID: 35255283
J Orthop Translat

2026 Jul 23:60:101173. PMID: 42540370
BMC Med

NLRC5 exerts anti-endometriosis effects through inhibiting ERβ-mediated inflammatory response. [Abstract]

2024 Sep 2;22(1):351. PMID: 39218863
Environ Pollut

BPA modulates the WDR5/TET2 complex to regulate ERβ expression in eutopic endometrium and drives the development of endometriosis. [Abstract]

2021 Jan 1;268(Pt B):115748. PMID: 33022573
Front Immunol

Estrogen Acts Through Estrogen Receptor-β to Promote Mannan-Induced Psoriasis-Like Skin Inflammation. [Abstract]

2022 May 19;13:818173. PMID: 35663991
mLife

The synthetic estradiol analog E0703 enhances Akkermansia muciniphila growth for radiation-induced intestinal damage repair. [Abstract]

2026 Apr 30;5(2):199-216. PMID: 42079447
J Agric Food Chem

Zearalenone Induces Estrogen-Receptor-Independent Neutrophil Extracellular Trap Release in Vitro. [Abstract]

2019 Apr 24;67(16):4588-4594. PMID: 30939243
Ecotoxicol Environ Saf

Bisphenol A interferes with lncRNA Fhadlos2 and RUNX3 association in adolescent mouse ovary. [Abstract]

2023 Jul 1:259:115060. PMID: 37229876
Ecotoxicol Environ Saf

Effect of bisphenol A on craniofacial cartilage development in zebrafish (Danio rerio) embryos: A morphological study. [Abstract]

2021 Apr 1:212:111991. PMID: 33548570
Biochem Pharmacol

Estradiol alleviated chemotherapy-induced premature ovarian failure by blocking the ferroptosis via activating ESR2/Sirt1/Nrf2 pathway. [Abstract]

2025 Oct 29;243(Pt 1):117481. PMID: 41173058
Biochem Pharmacol

MICAL-L2, as an estrogen-responsive gene, is involved in ER-positive breast cancer cell progression and tamoxifen sensitivity via the AKT/mTOR pathway. [Abstract]

2024 Jul:225:116256. PMID: 38729448
Life Sci

Genistein accelerates glucose catabolism via activation the GPER-mediated cAMP/PKA-AMPK signaling pathway in broiler chickens. [Abstract]

2022 Aug 15:303:120676. PMID: 35640778
Nutrients

Genistein Regulates Lipid Metabolism via Estrogen Receptor β and Its Downstream Signal Akt/mTOR in HepG2 Cells. [Abstract]

2021 Nov 10;13(11):4015. PMID: 34836271
Eur J Pharmacol

Estradiol reduced 5-HT reuptake by downregulating the gene expression of Plasma Membrane Monoamine Transporter (PMAT, Slc29a4) through estrogen receptor β and the MAPK/ERK signaling pathway. [Abstract]

2022 Jun 5;924:174939. PMID: 35398393
Eur J Pharmacol

Arctigenin inhibits abnormal germinal center reactions and attenuates murine lupus by inhibiting IFN-I pathway. [Abstract]

2022 Mar 15:919:174808. PMID: 35151645
Eur J Pharmacol

Syringaresinol attenuates sepsis-induced cardiac dysfunction by inhibiting inflammation and pyroptosis in mice. [Abstract]

2021 Dec 15:913:174644. PMID: 34801532
Int J Mol Sci

Emodin Promoted Intestinal Secretion of GLP-1 and Limited Cognitive Deficits in Young Bilateral Ovariectomized Rats. [Abstract]

2026 Apr 10;27(8):3414. PMID: 42074060
Biomolecules

Active Estrogen-Succinate Metabolism Promotes Heme Accumulation and Increases the Proliferative and Invasive Potential of Endometrial Cancer Cells. [Abstract]

2023 Jul 10;13(7):1097. PMID: 37509133
J Clin Endocrinol Metab

Organoid Cultures Derived From Patients With Papillary Thyroid Cancer. [Abstract]

2021 Apr 23;106(5):1410-1426. PMID: 33524147
Biol Sex Differ

Membrane-associated estrogen receptor α prevents the amyloid β-induced suppression of GIRK channel activity in hippocampal neurons from female mice. [Abstract]

2025 Nov 6;16(1):90. PMID: 41199341
Molecules

Apigenin Inhibits Histamine-Induced Cervical Cancer Tumor Growth by Regulating Estrogen Receptor Expression. [Abstract]

2020 Apr 23;25(8):1960. PMID: 32340124
Sci Rep

Oroxylin A may promote cell apoptosis and inhibit epithelial-mesenchymal transition in endometrial cancer, associated with the ERβ/PI3K/AKT pathway. [Abstract]

2025 Apr 10;15(1):12225. PMID: 40211010
J Cell Mol Med

17-β-Estradiol Protects Chondrocytes From Senescence and Ameliorates Osteoarthritis Progression via ERα-AKT-FOXO4 Pathway. [Abstract]

2026 Feb;30(3):e71018. PMID: 41677002
J Pharm Pharmacol

Formononetin attenuates corticosterone-induced depressive-like behaviors and neuronal damage via ERα/ERK-CREB-BDNF signaling pathway. [Abstract]

2026 Feb 7;78(2):rgag010. PMID: 41697882
Food Chem Toxicol

The environmental estrogen Bisphenol (A) enhances lung cancer progression in vitro and in vivo in presence of estradiol by targeting PI3k/Akt pathway. [Abstract]

2026 Jun 2:215:116197. PMID: 42235672
Hum Fertil (Camb)

Effects of E2/ERβ on follicular granulosa cells and on AMH/Smad signalling in endometriosis. [Abstract]

2026 Dec;29(1):2638250. PMID: 41789475
Neurourol Urodyn

Estrogen inhibits bladder overactivity in rats with cyclophosphamide-induced cystitis via downregulating the expression of P2X3 receptors in bladder epithelium cells. [Abstract]

2022 Jan;41(1):174-187. PMID: 34622458
Eur J Inflamm

October 11, 2021.
SSRN

2024 Jan 16.

Lösungsmittel & Löslichkeit

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

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.

Molaritätsrechner

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

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

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

Stock Solution Working Solution

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.

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.

Protocol 3

Add each solvent one by one: 50% PEG400 50% Saline

Solubility: 1.67 mg/mL (3.95 mM); Suspended solution; Need ultrasonic

Working Solution

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 Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Protokoll

All Signal Pathway Related

Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (281 KB)
SDS (480 KB)
- English - EN (480 KB)
- Français - FR (480 KB)
- Deutsch - DE (480 KB)
- Norwegian - NO (480 KB)
- Español - ES (480 KB)
- Swedish - SV (480 KB)
- Italian - IT (480 KB)
- Korean - KR (480 KB)
- Portuguese - PT (480 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Dennis R Compton, 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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Bioz

Keywords

PHTPP

34 Cited Publications

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PHTPP

Publications Citing Use of MedChemExpress (MCE) PHTPP

Alle Estrogen Receptor/ERR Isoform-spezifische Produkte anzeigen