Biological Activity
Potent GABAA antagonist (Ki = 0.0028 μM at rat GABAA receptors; IC50 = 0.024 μM at human α1β2γ2 GABAA-expressing tsA201 cells). Displays no inhibitory activity at hGAT-1, hGAT-2, hGAT-3 or hBGT-1 GABA transporters.
Compound Libraries
PHP 501 trifluoroacetate is also offered as part of the Tocriscreen Plus. Find out more about compound libraries available from Tocris.
Technical Data
| M. Wt | 433.42 |
| Formula | C20H21N3O.CF3CO2H |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1236105-75-1 |
| PubChem ID | 90488945 |
| InChI Key | SULXXKLCQRXMHP-UHFFFAOYSA-N |
| Smiles | ON1N=CC(C3CCNCC3)=C1C2=CC=CC(C4=CC=CC=C4)=C2.FC(F)(C(O)=O)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 | 43.34 | 100 | |
| ethanol | 4.33 | 10mM with gentle warming |
Preparing Stock Solutions
The following data is based on the product molecular weight 433.42. 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 | 2.31 mL | 11.54 mL | 23.07 mL |
| 5 mM | 0.46 mL | 2.31 mL | 4.61 mL |
| 10 mM | 0.23 mL | 1.15 mL | 2.31 mL |
| 50 mM | 0.05 mL | 0.23 mL | 0.46 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Møller et al (2010) Novel 4-(piperidin-4-yl)-1-hydroxypyrazoles as gamma-aminobutyric acid(A) receptor ligands: synthesis, pharmacology, and structure-activity relationships. J.Med.Chem. 53 3417 PMID: 20355712
Keywords: PHP 501 trifluoroacetate, supplier, GABAA, receptors, antagonists, potent, PHP501, GABAA, Receptors, GABAA, Receptors, Tocris Bioscience
