TABLE 1

Selectivity of SKA-111 and SKA-121 over selected ion channels

The number in parentheses indicates the number of cells used to determining the EC50 values or the % of current inhibition.

ChannelSKA-111 EC50SKA-121 EC50
KCa1.1120% of current at 25 µM (3)115% of current at 50 µM (3)
KCa2.18.1 ± 0.4 (10)8.7 ± 1.6 (8)
KCa2.27.7 ± 1.9 (10)6.8 ± 1.7 (12)
KCa2.313.7 ± 6.9 (15)4.4 ± 2.6 (18)
KCa3.10.111 ± 0.027 (24)0.019 ± 0.014 (21)
ChannelSKA-111% current inhibition at 25 µMSKA-121% current inhibition at 50 µM
KV1.328.5 ± 2.3% (4)27.5 ± 7.2% (3)
KV2.137.3 ± 9.0% (4)43.2 ± 12.5% (3)
KV3.132.9 ± 1.3% (3)46.3 ± 16.5% (4)
KV11.1 (hERG)10.1 ± 7.7% (5)16.7 ± 9.7% (5)
NaV1.219.5 ± 6.9% (5)15.2 ± 12.7% (5)
NaV1.433.4 ± 10.5% (5)25.7 ± 1.3% (5)
NaV1.539.9 ± 11.1% (5)32.1 ± 11.1% (5)
NaV1.727.5 ± 0.9% (3)28.5 ± 1.8% (5)
CaV1.249.5 ± 17.0% (5)48.9 ± 2.7% (5)