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CiPA panel

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Nav1.5

Time2020-04-20 14:24:04 Hits216


Nav1.5 is one of the voltage-gated sodium channels. The majority of sodium channels distributed in the heart is Nav1.5. The current mediated by Nav1.5 rapidly depolarizes cardiac myocytes, underlining the electrophysiological mechanism in the upstroke phase (phase 0) of cardiac action potential. Many congenital heart diseases such as Long QT syndrome 3, Brugada syndrome, sick sinus syndrome are caused by Nav1.5 mutation.

PharmaCore Labs provides manual patch clamp human Nav1.5 (hNav1.5) assay to evaluate drug's inhibition or potentiation effect on hNav1.5 channel.

In vitro electrophysiology hNav1.5 assay with manual patch clamp:

Assay platform/method

Conventional patch clamp

Cells used in the assay

HEK293 hNav1.5 stable cell line

Measured parameters

Whole cell current of hNav1.5 channels

Test concentrations

5 doses for IC50

Data point repeats

N ≥ 3 for each concentration

Note: Positive control: 10 μM Amitriptyline is used in the assay to ensure cell quality and normal response.




Current-time plot reflecting effect of amitriptyline on  the hNav1.5

Effectof different concentrations of amitriptyline on the

current-voltage (I-V) relationship on hNav1.5




Inhibition effect of amitriptyline on hNav1.5 at different inactivation state

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