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Description: Potent GABAA antagonist
Chemical Name: 4-(5-[1,1'-Biphenyl]-3-yl-1-hydroxy-1H-pyrazol-4-yl)piperidine trifluoroacetate
Purity: ≥98% (HPLC)
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.
Technical Data
| M. Wt | 433.42 |
| Formula | C20H21N3O.CF3CO2H |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1781880-44-1 |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 43.34 | 100 |
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 the degree 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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References
References are publications that support the biological activity of the product.
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
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Keywords: PHP 501 trifluoroacetate, PHP 501 trifluoroacetate supplier, GABAA, receptors, antagonists, potent, PHP501, Receptors, 4466, Tocris Bioscience
1 Citation for PHP 501 trifluoroacetate
Citations are publications that use Tocris products. Selected citations for PHP 501 trifluoroacetate include:
León et al (2016) Direct actions of kisspeptins on GnRH neurons permit attainment of fertility but are insufficient to fully preserve gonadotropic axis activity. Sci.Rep. 6 19206 PMID: 26755241
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