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Ionic channel assays : channel protein of human heart in vitro

Channels are stably transfected in HEK-293-cells.

OPTIONS: Room temperature or 35°C

 

1. hERG assays on Human Embryonic Kidney (HEK) cells: REGULATORY CHANNEL (ICHS7B)

Mutation LQT2: LONG QT

Standard hERG assay protocol:

• 6 treated cells and 6 control cells
  
• 3 or 4 increasing cumulative concentrations of assay compound
  
• Depolarizing protocol:

 

 

 

 

2. hERG trafficking inhibition on Human Embryonic Kidney (HEK) cells

HEK-293 long term exposure (24h) to the drug may have an indirect effect through inhibition of hERG protein trafficking from the endoplasmic reticulum to the cell surface.
→ REDUCTION OF THE SURFACE EXPRESSION OF THE FUNCTIONAL CARDIAC POTASSIUM hERG CHANNEL

3. hNa_V1.5 assays on Human Embryonic Kidney (HEK) cells (LQT3)

Mutation LQT3: LONG QT

Reference compound: flecainide

4. hK_VLQT1 assays on Human Embryonic Kidney (HEK) cells:

Channel involved in the slow component of the repolarisation of the action potential.

Mutation LQT1: LONG QT

5. hCa_V1.2 assays on Chinese Hamster Ovary (CHO) cells:

Reference compound: verapamil, nifedipine