Biological Activity
Selective estrogen ERβ receptor antagonist that displays 36-fold selectivity over ERα. Exhibits full antagonism at ERβ in a cotransfection assay in human endometrial cancer cells (HEC-1), with minimal effects on ERα.
Compound Libraries
PHTPP is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 423.31 |
| Formula | C20H11F6N3O |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 805239-56-9 |
| PubChem ID | 11201035 |
| InChI Key | AEZPAUSGTAHLOQ-UHFFFAOYSA-N |
| Smiles | OC1=CC=C(C=C1)C1=C2N=C(C=C(N2N=C1C1=CC=CC=C1)C(F)(F)F)C(F)(F)F |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 13.96 | 33 | |
| ethanol | 42.33 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 423.31. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 2.36 mL | 11.81 mL | 23.62 mL |
| 5 mM | 0.47 mL | 2.36 mL | 4.72 mL |
| 10 mM | 0.24 mL | 1.18 mL | 2.36 mL |
| 50 mM | 0.05 mL | 0.24 mL | 0.47 mL |
Molarity Calculator
Reconstitution Calculator
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Product Datasheets
References
References are publications that support the products' biological activity.
Compton et al (2004) Pyrazolo[1,5-a]pyrimidines: estrogen receptor ligands possessing estrogen receptor β antagonist activity. J.Med.Chem. 47 5872 PMID: 15537344
Compton et al (2005) Erratum. J.Med.Chem. 48 2724 PMID:
Keywords: PHTPP, supplier, Selective, ERβ, ERbeta, antagonists, Estrogen, Receptors, Estrogen, and, Related, Receptors, Estrogen, and, Related, Receptors, Tocris Bioscience
