Biological Activity
Positive allosteric modulator of AMPA receptors (Ki = 85 nM). Prevents ketamine-induced working memory impairments. Brain penetrant.
Licensing Information
Sold for research purposes under agreement from Pfizer Inc.
Technical Data
| M. Wt | 390.52 |
| Formula | C19H22N2O3S2 |
| Storage | Store at +4°C |
| Purity | ≥98% (HPLC) |
| CAS Number | 1219633-99-4 |
| PubChem ID | 44462786 |
| InChI Key | FFAGHPLLBXWCSF-MSOLQXFVSA-N |
| Smiles | O=S(N[C@H]1CCOC[C@@H]1[C@]2=CC=C(C3=CC=C(C#N)S3)C=C2)(C(C)C)=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 | 39.05 | 100 | |
| ethanol | 19.53 | 50 |
Preparing Stock Solutions
The following data is based on the product molecular weight 390.52. 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 | 2.56 mL | 12.8 mL | 25.61 mL |
| 5 mM | 0.51 mL | 2.56 mL | 5.12 mL |
| 10 mM | 0.26 mL | 1.28 mL | 2.56 mL |
| 50 mM | 0.05 mL | 0.26 mL | 0.51 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Roberts et al (2010) Prevention of ketamine-induced working memory impairments by AMPA potentiators in a nonhuman primate model of cognitive dysfunction. Behav.Brain Res. 212 41 PMID: 20347881
Doran et al (2012) An evaluation of using rat-derived single-dose neuropharmacokinetic parameters to project accurately large animal unbound brain drug concentrations. Drug Metab.Dispos. 40 2162 PMID: 22899853
Shaffer et al (2013) Positive allosteric modulation of AMPA receptors from efficacy to toxicity: the interspecies exposure-response continuum of the novel potentiator PF-4778574. J.Pharmacol.Exp.Ther. 347 212 PMID: 23899905
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