Size | Price | Stock | Qty |
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25mg |
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50mg |
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100mg |
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250mg |
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500mg |
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Other Sizes |
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Purity: ≥98%
PHTPP is an estrogen receptor (ERβ) antagonist. It exhibits 36-fold selectivity for ERβ relative to ERα. PHTPP has no effect on basal cAMP production but reduces FSH-mediated cAMP production by 80%. PHTPP does not suppress E2-stimulated ERα activity, but it does inhibit E2-stimulated ERβ activity (at a concentration of 10-6 M). When taken in large quantities, PHTPP both promotes and modestly elevates the expression of class 1 Igf1 mRNA in response to DPN.
Targets |
ERβ
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ln Vitro |
PHTPP shows no appreciable agonism on ERα or Erβ, but is completely effective as an ERβ antagonist[1]. PHTPP treatment inhibits the growth and invasion of bladder cancer (BCa) cells as well as the expression of MCM5[2].
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ln Vivo |
PHTPP can prevent the growth and invasion of bladder cancer, improving the survival rate in a mouse model of bladder cancer induced by the carcinogen N-butyl-N-(4-hydroxybutyl) nitrosamine (BBN)[2].
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Cell Assay |
For 24 hours, HEK 293 cells are cultured in DMEM enhanced with 10% fetal bovine serum stripped of charcoal. Subsequently, the cells are transfected with the Erβ expressing vector (pcDNA3-ERβ), the estrogen response element (ERE) firefly luciferase reporter, and the SV40-driven renilla expressing vector as a control. After 8 hours, DMSO or 10 nM 2,3-bis(4-hydroxyphenyl)-propionitrile (DPN) with varying concentrations of PHTPP are added. Cells are lysed with lysis buffer and analyzed after a 24-hour period.
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Animal Protocol |
Female B6 mice
10 μl of 10 mM PHTPP per mouse i.p. |
References |
Molecular Formula |
C20H11F6N3O
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Molecular Weight |
423.31
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Exact Mass |
423.08
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Elemental Analysis |
C, 56.75; H, 2.62; F, 26.93; N, 9.93; O, 3.78
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CAS # |
805239-56-9
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
C1=CC=C(C=C1)C2=NN3C(=CC(=NC3=C2C4=CC=C(C=C4)O)C(F)(F)F)C(F)(F)F
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InChi Key |
AEZPAUSGTAHLOQ-UHFFFAOYSA-N
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InChi Code |
InChI=1S/C20H11F6N3O/c21-19(22,23)14-10-15(20(24,25)26)29-18(27-14)16(11-6-8-13(30)9-7-11)17(28-29)12-4-2-1-3-5-12/h1-10,30H
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Chemical Name |
4-[2-phenyl-5,7-bis(trifluoromethyl)pyrazolo[1,5-a]pyrimidin-3-yl]phenol
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
J Med Chem.2004 Nov 18;47(24):5872-93. th> |
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ERβ antagonist, PHTPP, reduced MCM5 expression and BCa cell growth and invasion by inhibiting ERβ transactivation and expression of target gene,MCM5.Carcinogenesis.2014Mar;35(3):651-61. td> |