Biological Activity
Novel allosteric potentiator of AMPA receptor desensitization. Slows the rate of onset of desensitization and potentiates steady-state equilibrium currents induced by glutamate with subunit (GluR3/4 > GluR1) and splice variant (flop > flip) selectivity. Ameliorates post-ischemic memory impairment in rats following i.v. administration.
Technical Data
| M. Wt | 402.44 |
| Formula | C16H16F2N2O4S2 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 141286-78-4 |
| PubChem ID | 6603828 |
| InChI Key | GTACSIONMHMRPD-UHFFFAOYSA-N |
| Smiles | FC1=CC(SCCNS(C2=CC=CC=C2)(=O)=O)=CC(F)=C1OCC(N)=O |
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 | 40.24 | 100 | |
| ethanol | 10.06 | 25 |
Preparing Stock Solutions
The following data is based on the product molecular weight 402.44. 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 | 2.48 mL | 12.42 mL | 24.85 mL |
| 5 mM | 0.5 mL | 2.48 mL | 4.97 mL |
| 10 mM | 0.25 mL | 1.24 mL | 2.48 mL |
| 50 mM | 0.05 mL | 0.25 mL | 0.5 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Sekiguchi et al (1997) A novel allosteric potentiator of AMPA receptors: 4-[2-(phenylsulfonylamino)ethylthio]-2,6-difluoro-phenoxyacetamide. J.Neurosci. 17 5760 PMID: 9221774
Sekiguchi et al (2002) A desensitization-selective potentiator of AMPA-type glutamate receptors. Br.J.Pharmacol. 136 1033 PMID: 12145103
Sekiguchi et al (2001) The AMPA receptor allosteric potentiator PEPA ameliorates post-ischemic memory impairment. Neuroreport 12 2974 PMID:
Keywords: PEPA, supplier, Allosteric, potentiator, AMPA, receptor, desensitization, desensitisation, Glutamate, Receptors, iGluR, Ionotropic, AMPA, Receptors, AMPA, Receptors, Tocris Bioscience
