| Assay Method Information | |
| | Biological Assay |
| Description: | To assess peak Nav1.5 current inhibition in an atrial fibrillation-mimicking condition (Nav1.5 IC50 (5 Hz, AF-like rate) (μM)), compounds were first prepared at 10 mM in DMSO, and cells were pre-incubated with test compounds at each concentration for 3 min. in an ascending order of 0, 0.37, 1.1, 3.3, 10 and 30 μM. An atrial action potential-like protocol consisting of a voltage ramp (+10 mV to −85 mV for a 150 ms duration and a holding potential at −85 mV) was then applied to cells at 5 Hz for 12 s until no further current change or inhibition was observed. The percent inhibition (expressed as ([Iafter compound treatment/Ibefore compound treatment]×100%) is calculated by normalizing the peak current amplitude at the last pulse of each of the 6 compound concentrations by the amplitude before exposure to the test compound. |
| Affinity data for this assay | |
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