Biological Activity
Potent, subtype-selective estrogen receptor agonist (EC50 ~ 200 pM); displays 410-fold selectivity for ERα over ERβ. Prevents ovariectomy-induced weight gain and loss of bone mineral density, and induces gene expression in the hypothalamus following systemic administration in vivo.
Compound Libraries
PPT is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 386.45 |
| Formula | C24H22N2O3 |
| Storage | Store at +4°C |
| Purity | ≥99% (HPLC) |
| CAS Number | 263717-53-9 |
| PubChem ID | 6095481 |
| InChI Key | UOSWGERPQQOSHS-UHFFFAOYSA-N |
| Smiles | CCCC1=C(N(N=C1C1=CC=C(O)C=C1)C1=CC=C(O)C=C1)C1=CC=C(O)C=C1 |
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 | 38.65 | 100 | |
| ethanol | 1.93 | 5 |
Preparing Stock Solutions
The following data is based on the product molecular weight 386.45. 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 | 2.59 mL | 12.94 mL | 25.88 mL |
| 5 mM | 0.52 mL | 2.59 mL | 5.18 mL |
| 10 mM | 0.26 mL | 1.29 mL | 2.59 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.52 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Harris et al (2002) Characterization of the biological roles of the estrogen receptors, ERα and ERβ, in estrogen target tissues in vivo through the use of an ERα-selective ligand. Endocrinology 143 4172 PMID: 12399409
Kraichely et al (2000) Conformational changes and coactivator recruitment by novel ligands for estrogen receptor-α and estrogen receptor-β: correlations with biological character and distinct differences among SRC coactivator family members. Endocrinology 141 3534 PMID: 11014206
Stauffer et al (2000) Pyrazole ligands: structure-affinity/activity relationships and estrogen receptor-α-selective agonists. J.Med.Chem. 43 4934 PMID: 11150164
Keywords: PPT, supplier, Subtype-selective, ERα, ERalpha, agonists, ERR, Estrogen, Receptors, Estrogen, and, Related, Receptors, Estrogen, and, Related, Receptors, Tocris Bioscience
