PHTPP
Based on 33 publication(s) in Google Scholar
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.
- Purity: 99.56%
- CAS No.: 805239-56-9
- Formula: C20H11F6N3O
- Molecular Weight:423.31
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Protocol
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) PHTPP
More- Cell Mol Biol Lett. 2025 Nov 13;30(1):136. [Abstract]
- Int J Biol Sci. 2024 Mar 25;20(6):2236-2260. [Abstract]
- Phytomedicine. 2026 Apr:153:157917. [Abstract]
- Phytomedicine. 2024 Jan:123:155218. [Abstract]
- Phytomedicine. 2023 Jul:115:154839. [Abstract]
- Phytomedicine. 2022 May:99:154022. [Abstract]
- BMC Med. 2024 Sep 2;22(1):351. [Abstract]
- Environ Pollut. 2021 Jan 1;268(Pt B):115748. [Abstract]
- Front Immunol. 2022 May 19;13:818173. [Abstract]
- mLife. 2026 Apr 30;5(2):199-216. [Abstract]
- J Agric Food Chem. 2019 Apr 24;67(16):4588-4594. [Abstract]
- Ecotoxicol Environ Saf. 2023 Jul 1:259:115060. [Abstract]
- Ecotoxicol Environ Saf. 2021 Apr 1:212:111991. [Abstract]
- Biochem Pharmacol. 2025 Oct 29;243(Pt 1):117481. [Abstract]
- Biochem Pharmacol. 2024 Jul:225:116256. [Abstract]
- Life Sci. 2022 Aug 15:303:120676. [Abstract]
- Nutrients. 2021 Nov 10;13(11):4015. [Abstract]
- Eur J Pharmacol. 2022 Jun 5;924:174939. [Abstract]
- Eur J Pharmacol. 2022 Mar 15:919:174808. [Abstract]
- Eur J Pharmacol. 2021 Dec 15:913:174644. [Abstract]
- Int J Mol Sci. 2026 Apr 10;27(8):3414. [Abstract]
- Biomolecules. 2023 Jul 10;13(7):1097. [Abstract]
- J Clin Endocrinol Metab. 2021 Apr 23;106(5):1410-1426. [Abstract]
- Biol Sex Differ. 2025 Nov 6;16(1):90. [Abstract]
- Molecules. 2020 Apr 23;25(8):1960. [Abstract]
- Sci Rep. 2025 Apr 10;15(1):12225. [Abstract]
- J Cell Mol Med. 2026 Feb;30(3):e71018. [Abstract]
- J Pharm Pharmacol. 2026 Feb 7;78(2):rgag010. [Abstract]
- Food Chem Toxicol. 2026 Jun 2:215:116197. [Abstract]
- Hum Fertil (Camb). 2026 Dec;29(1):2638250. [Abstract]
- Neurourol Urodyn. 2022 Jan;41(1):174-187. [Abstract]
- Eur J Inflamm. October 11, 2021.
- SSRN. 2024 Jan 16.
Customer Validation & Images
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Cell Imaging/Staining
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Flow Cytometry
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WB
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Cell Imaging/Staining
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Flow Cytometry
Biological Activity
ERβ[1]
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.
Chemical Information
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CAS No. 805239-56-9
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Appearance Solid
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Molecular Weight 423.31
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Formula C20H11F6N3O
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Color Light yellow to yellow
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SMILES
OC1=CC=C(C2=C3N=C(C(F)(F)F)C=C(C(F)(F)F)N3N=C2C4=CC=CC=C4)C=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (33)
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Journal Impact Factor
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Most Recent
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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.
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Int J Biol Sci
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.
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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.
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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 -
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
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 -
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Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Add each solvent one by one: 50% PEG400 50% Saline
Solubility: 1.67 mg/mL (3.95 mM); Suspended solution; Need ultrasonic
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.
Add each solvent one by one: 15% Cremophor EL 85% Saline
Solubility: 5 mg/mL (11.81 mM); Suspended solution; Need ultrasonic
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Protocol
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Purity & Documentation
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Data Sheet (281 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
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 |
PHTPP Related Classifications
HY-103456 Related Classifications
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