Table 1. Patch clamp IC50 values for block of cardiac ion channels by Vx a.
Vx Concentration-Response Relationship | |||||
---|---|---|---|---|---|
Channel | Hz | Test Pulses / Minute | Cell Line | IC50 (μM) | |
| |||||
hKv11.1 (IKr) | 0.1 | 6 | HEK-293 | 0.00084 (n=3-8) |
|
| |||||
ICa,L | 0.05 | 3 | ventricular myocyte | 0.32 (n=2-4) |
|
| |||||
hCav3.2 | 0.1 | 6 | HEK-293 | 2.0 b | |
| |||||
hNav1.5 (INa) | 0.1 | 6 | HEK-293 | 0.83 (n=2-5) |
|
| |||||
hKv1.5 (IKur) | 0.1 | 6 | HEK-293 | 1.0 (n=2-3) |
|
| |||||
rKv4.3 | (Ito peak) | 0.067 | 4 | L | 9.8 |
(Ito 70 ms) | 0.067 | 4 | L | 2.0 (n=2-3) |
|
| |||||
hKv7.1/hKCNE1 (IKs) | 0.067 | 4 | CHO | 2.9 (n=3-5) |
Data from 2 or more cells were pooled for IC50 measurements; n indicates the range of replicates from all concentrations used to construct the IC50. See Figure 1 for n at each concentration for hKv11.1, ICa,L and hNav1.5.
Estimated IC50 from 83% block at 10 μM (n=2).