Biological Activity
Novel, potent, non-competitive AMPA receptor antagonist (IC50 = 2.8 μM ). Acts allosterically at the same regulatory site as GYKI 52466 and 53655 and other benzodiazepines but does not bind to the central diazepine binding site. Selective for AMPA relative to kainate receptor sub-types. Similar potency to GYKI 53655. Anticonvulsant in vivo.
Licensing Information
Sold with the permission of Annovis Inc.
Technical Data
| M. Wt | 366.42 |
| Formula | C20H22N4O3 |
| Storage | Store at RT |
| Purity | ≥99% (HPLC) |
| CAS Number | 173952-44-8 |
| PubChem ID | 5039877 |
| InChI Key | OFUDZKKOKPGXOH-UHFFFAOYSA-N |
| Smiles | CCCNC(=O)N1N=C(C2=CC=C(N)C=C2)C2=C(C=C3OCOC3=C2)C1C |
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 | 36.64 | 100 | |
| ethanol | 36.64 | 100 |
Preparing Stock Solutions
The following data is based on the product molecular weight 366.42. 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 | 2.73 mL | 13.65 mL | 27.29 mL |
| 5 mM | 0.55 mL | 2.73 mL | 5.46 mL |
| 10 mM | 0.27 mL | 1.36 mL | 2.73 mL |
| 50 mM | 0.05 mL | 0.27 mL | 0.55 mL |
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Product Datasheets
References
References are publications that support the products' biological activity.
Bleakman et al (2002) Kainate receptor agonists, antagonists and allosteric modulators. Curr.Pharm.Des. 8 873 PMID: 11945137
Pelletier et al (1996) Substituted 1,2-dihydrophthalazines: potent, selective and non-competitive inhibitors of the AMPA receptor. J.Med.Chem. 39 343 PMID: 8558499
Li et al (1999) Kainate-receptor-mediated sensory synaptic transmission in mammalian spinal cord. Nature 397 161 PMID: 9923678
Keywords: SYM 2206, supplier, Non-competitive, AMPA, antagonist, Glutamate, Receptors, iGlur, Ionotropic, SYM2206, AMPA, Receptors, AMPA, Receptors, Tocris Bioscience
