Biological Activity
Selective, non-competitive AMPA antagonist (IC50 = 25 nM in rat cortical neurons) that displays potent anticonvulsant activity. Also significantly blocks the persistent component of Nav1.6 channel activity. Brain penetrant and orally active.
Technical Data
| M. Wt | 499.41 |
| Formula | C26H24ClFN4O.HCl |
| Storage | Desiccate at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 199655-36-2 |
| PubChem ID | 53251536 |
| InChI Key | YKYDGCRJPYLXHY-GVYCEHEKSA-N |
| Smiles | O=C2N(C3=CC=CC=C3Cl)C(/C=C/C4=NC(CN(CC)CC)=CC=C4)=NC1=CC=C(F)C=C12.Cl |
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 | 49.94 | 100 | |
| water | 4.99 | 10 |
Preparing Stock Solutions
The following data is based on the product molecular weight 499.41. 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 mL | 10.01 mL | 20.02 mL |
| 5 mM | 0.4 mL | 2 mL | 4 mL |
| 10 mM | 0.2 mL | 1 mL | 2 mL |
| 50 mM | 0.04 mL | 0.2 mL | 0.4 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Lazaro et al (2002) Functional characterization of CP-465,022, a selective, noncompetitive AMPA receptor antagonist. Neuropharmacology 42 143 PMID: 11804610
Menniti et al (2003) CP-465,022, a selective noncompetitive AMPA receptor antagonist, blocks AMPA receptors but is not neuroprotective in vivo. Stroke 34 171 PMID: 12511770
Welch et al (2008) Traditional AMPA receptor antagonists partially block Nav1.6-mediated persistent current. Neuropharmacology 55 1165 PMID: 18687344
Keywords: CP 465022 hydrochloride, supplier, Selective, non-competitive, AMPA, antagonists, Glutamate, Receptors, iGluR, Ionotropic, CP465022, hydrochloride, AMPA, Receptors, AMPA, Receptors, Tocris Bioscience
