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hKVLQT1/​MinK

hKVLQT1 assays on Human Embry­onic Kid­ney (HEK) cells:

Since the hKVLQT1/​MinK chan­nel plays an impor­tant role in car­diac action poten­tial repo­lar­i­sa­tion, a phar­ma­co­log­i­cal reduc­tion of the IKs cur­rent may delay the repo­lar­i­sa­tion process and may lead to a pro­lon­ga­tion of the QT inter­val. Thus, the hKVLQT1/​MinK potas­sium chan­nel rep­re­sents a spe­cific tar­get for the car­diac safety assessment.

Muta­tion LQT1: LONG QT

Stim­u­la­tion pro­to­col:
  • Stim­u­la­tion fre­quency: 0.2 Hz


Mea­sured para­me­ters:
  • Ampli­tude of the tail cur­rent upon repo­lar­iza­tion to –40mV (pA)
  • Ampli­tude of the base cur­rent at –80mV (pA)
  • Inhi­bi­tion of hKVLQT1/​MinK tail cur­rent amplitude(%)
  • IC50 value
figure Iks Ref­er­ence com­pounds or pos­i­tive con­trols

REF­ER­ENCE

COM­POUNDS

IC50
Meflo­quine 0.7 µM
Chro­manol 293B 6.0 µM
XE-​991 1.5 µM