CP 465022 hydrochloride

Product details

• Chemical name: 3-(2-chlorophenyl)-2-[(E)-2-[6-(diethylaminomethyl)pyridin-2-yl]ethenyl]-6-fluoroquinazolin-4-one;hydrochloride.
• CAS number: 199655-36-2
• Molecular formula: C26H25Cl2FN4O.
• Purity: >97% (HPLC)
• Concentration: 25 nM - 25 µM.
• Form: Lyophilized powder.
• Solubility: >25 mM in DMSO. Centrifuge all product preparations before use.
• Reconstitution: >25 mM in DMSO. Centrifuge all product preparations before use.
• Shipping: Shipped at room temperature. Product as supplied can be stored intact at room temperature for several weeks. For longer periods, it should be stored at -20°C.
• Target: AMPA receptors, NaV1.6 Na+ channels
• Source: Synthetic
• Activity: CP 465022 is a selective, non-competitive AMPA receptor antagonist. It inhibits AMPA receptor-mediated currents in rat cortical neurons (IC50 25 nM)1. It also partially blocks the persistent components of NaV1.6 channel activity2.

Scientific background

CP 465022 hydrochloride is a selective, non-competitive antagonist of the AMPA receptor and a modulator of the voltage-gated sodium NaV1.6 channel. It has an IC50 value of 25 nM for AMPA mediated currents in rat cortical neurons and in human neuronal hNT cell lines, an IC50 of 15 nM can be observed. The inhibitory effect of CP develops slowly. The reversal of its inhibition is also slow upon compound washout, suggesting a slow rate of interaction between CP and the AMPA receptor. This may also be attributed to CP's high lypophilicity and protein binding. CP reduces the efficacy of kainate activation of AMPA receptors at any kainate concentration, indicating that it binds to a site other than the agonist site. Inhibition of the AMPA receptor by CP is neither use-dependent nor voltage-dependent1,2. CP significantly inhibits the persistent inward Na+ current of the NaV1.6 channel in a dose-dependent manner3. This requires caution when ascribing actions to the AMPA receptor based on CP.

Lead time: 1-2 Business Days

Country of origin: Israel/IL

Applications key

Application key: FC- Flow cytometry, IFC- Indirect flow cytometry, IHC- Immunohistochemistry,LCI- Live cell imaging, Calcium imaging assay,Cell survival assay, Electrophysiology, Neurite outgrowth assay.

Bioassay tested: Yes

• SDS (PDF)

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