Chemical Name: 3-(2-Chlorophenyl)-2-[2-[6-[(diethylamino)methyl]-2-pyridinyl]ethenyl]-6-fluoro-4(3H)-quinazolinone hydrochloride
Purity: ≥99% (HPLC)
Biological Activity
Technical Data
Solubility
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References
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.
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
Certificate of Analysis / Product Datasheet
Safety Datasheet
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References
References are publications that support the products' biological activity.
Lazaroet al (2002) Functional characterization of CP-465,022, a selective, noncompetitive AMPA receptor antagonist. Neuropharmacology 42 143 PMID: 11804610
Mennitiet 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
Welchet al (2008) Traditional AMPA receptor antagonists partially block Nav1.6-mediated persistent current. Neuropharmacology 55 1165 PMID: 18687344