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hNaV1.5

hNaV1.5 assays on Human Embry­onic Kid­ney (HEK) cells

Since the NaV1.5 chan­nel plays an impor­tant role in car­diac action poten­tial depo­lar­i­sa­tion (dV/​dtmax), a phar­ma­co­log­i­cal reduc­tion of this sodium cur­rent may delay the depo­lar­i­sa­tion process and may lead to a reduc­tion of the car­diac con­duc­tion. This makes the human NaV1.5 sodium chan­nel a tar­get for the car­diac safety assessment.

Muta­tion LQT3: LONG QT

Stim­u­la­tion pro­to­col:
  • GLP com­pli­ant
  • man­ual patch-​clamp technique
  • stim­u­la­tion fre­quency: 0.2 Hz


Mea­sured para­me­ters:
  • Ampli­tude of the peak cur­rent upon depo­lar­iza­tion to –30mV (pA)
  • Ampli­tude of the base cur­rent at –110mV (pA)
  • Inhi­bi­tion of NaV1.5 peak cur­rent amplitude (%)
  • IC50 value
Ref­er­ence com­pounds or pos­i­tive con­trols

REF­ER­ENCE

COM­POUNDS

IC50
Fle­caïnide 32.3 nM
quini­dine 21.1 nM