PHTPP |
Catalog No.GC11863
One-Click Copy Product Info
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PHTPP is a selective ERβ full antagonist with 36-fold selectivity for ERβ over ERα. PHTPP can selectively antagonize the ligand binding and transcriptional functions of ERβ, blocking its inhibitory effect on tumor cells, thereby promoting cell proliferation. PHTPP was used to verify ERβ function.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 805239-56-9
Sample solution is provided at 25 µL, 10mM.
PHTPP is a selective ERβ full antagonist with 36-fold selectivity for ERβ over ERα. PHTPP can selectively antagonize the ligand binding and transcriptional functions of ERβ, blocking its inhibitory effect on tumor cells, thereby promoting cell proliferation. PHTPP was used to verify ERβ function [1-3].
In MCF-7 cells, PHTPP (5μM, 1h) significantly weakened the inhibitory effect of silibinin on MCF-7 breast cancer cells by blocking the activity of ERβ [4]. In Caco-2 cells, PHTPP (0.1μM, 24h) reversed the p-hydroxybenzoic acid-induced inhibition of the expression of proinflammatory factors (e.g., TNF-α and IL-6) and upregulated the expression of E-cadherin and occluding [5]. In SKOV3 cells, PHTPP (10μM, 24h) promotes the proliferation and migration of SKOV3 cells [6].
In colitis mouse model, PHTPP (1mg/kg, ip, 1d) reversed the improvement effect of p-hydroxybenzoic acid on the symptoms of colitis [5]. In sprague-dawley rat model, PHTPP (0.091mg/kg, sc, 12 weeks) could block the antifibrotic effects of E2 [7]. In sprague-dawley rat model, PHTPP (850μg/kg, ip, 12d) inhibited ERβ activation by E2 and naringenin by over 90% [8].
References:
[1]. Compton DR, Sheng S, Carlson KE, et al. Pyrazolo [1, 5-a] pyrimidines: estrogen receptor ligands possessing estrogen receptor β antagonist activity. Journal of medicinal chemistry. 2004 Nov 18; 47(24): 5872-5893.
[2]. Chan KK, Leung TH, Chan DW, et al. Targeting estrogen receptor subtypes (ERa and ERb) with selective ER modulators in ovarian cancer. J. Endocrinol. 2014; 221: 325-336.
[3]. Boopathy GT, Hong W. Role of hippo pathway-YAP/TAZ signaling in angiogenesis. Frontiers in cell and developmental biology. 2019 Apr 10; 7: 49.
[4]. Zheng N, Liu L, Liu W, et al. ERβ up-regulation was involved in silibinin-induced growth inhibition of human breast cancer MCF-7 cells. Archives of biochemistry and biophysics. 2016 Feb 1; 591: 141-149.
[5]. Xu X, Luo A, Lu X, et al. p-Hydroxybenzoic acid alleviates inflammatory responses and intestinal mucosal damage in DSS-induced colitis by activating ERβ signaling. Journal of Functional Foods. 2021 Dec 1; 87: 104835.
[6]. Yan Y, Jiang X, Zhao Y, et al. Role of GPER on proliferation, migration and invasion in ligand‐independent manner in human ovarian cancer cell line SKOV3. Cell biochemistry and function. 2015 Dec; 33(8): 552-559.
[7]. Zhang B, Zhang CG, Ji LH, et al. Estrogen receptor β selective agonist ameliorates liver cirrhosis in rats by inhibiting the activation and proliferation of hepatic stellate cells. Journal of Gastroenterology and Hepatology. 2018 Mar; 33(3): 747-755.
[8]. Lin P, Zhang X, Zhu B, et al. Naringenin protects pancreatic β cells in diabetic rat through activation of estrogen receptor β. European Journal of Pharmacology. 2023 Dec 5; 960: 176115.
| Cell experiment [1]: | |
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Cell lines |
MCF-7 cells |
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Preparation Method |
MCF-7 cells were cultured in Minimum Essential Medium. All media were supplemented with 10% fetal bovine serum (FBS), penicillin (100U/mL) and streptomycin (100mg/mL). The cells were pre-treated with 5μM selective ERβ full antagonist (PHTPP) for 1h. |
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Reaction Conditions |
5μM; 1h |
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Applications |
PHTPP significantly weakened the inhibitory effect of silibinin on MCF-7 breast cancer cells by blocking the activity of Erβ. |
| Animal experiment [2]: | |
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Animal models |
Sprague-dawley rat model |
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Preparation Method |
Ninety female Sprague-Dawley rats, weighing 186±15g with an average age of approximately 8 weeks, were housed in a temperature and humidity-controlled environment with 12h light dark cycles and free access to food and water. The rats were randomly divided as follows into 9 groups of 10 rats each: Control, Carbon tetrachloride (CCl4), CCl4+E2, CCl4+PPT, CCl4+DPN, CCl4+G1, CCl4+E2+MPP, CCl4+E2+PHTPP and CCl4+E2+G15. The Control group underwent sham surgery, while the other 8 groups underwent bilateral ovariectomy. Two weeks after the surgeries, the 8 CCl4 groups were subcutaneously injected with 40% CCl4 in peanut oil at a dose of 0.2mL/100g body weight twice weekly. 5% alcohol was added to drinking water to induce P450 and intensify the development of hepatic fibrosis. Starting from the first CCl4 injection day, the rats received subcutaneously injections of the corresponding drugs (E2, PPT, DPN, G1, MPP, PHTPP and G15; first dissolved in DMSO and then diluted with saline) at a dosage of 30nM/100g body weight/day for 12 weeks, according to the grouping classification. The Control and CCl4 groups were treated subcutaneously with the same volume of placebos (peanut oil and/or DMSO diluted with saline). |
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Dosage form |
0.091mg/kg; sc; 12 weeks |
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Applications |
PHTPP could block the antifibrotic effects of E2. |
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References: |
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| 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 -20°C |
| 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. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.3623 mL | 11.8117 mL | 23.6233 mL |
| 5 mM | 472.5 μL | 2.3623 mL | 4.7247 mL |
| 10 mM | 236.2 μL | 1.1812 mL | 2.3623 mL |
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Working concentration: mg/ml;
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 saline, 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.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 23 reference(s) in Google Scholar.)