NS309

Description: NS309 is a nonselective activator of small- and intermediate-conductance Ca2+-activated K+ (SK/KCa2 and IK/KCa3.1) channels (EC50s range from 0.12-1.2 µM for SK channels and 10-90 nM for IK channels). It can also activate voltage-gated Kv11.1 channels (hERG, IC50 = 1 µM), but does not, however, affect large conductance (BK/KCa1.1) channels. NS309 can modulate neuronal firing patterns by enhancing SK-mediated hyperpolarizing effects. It is 730-fold (SK channels) and 7,400-fold (IK channels) more potent than 1-EBIO and often used in conjunction with CyPPA to distinguish between SK1 and SK3 subtypes. Target: Potassium Channel, EGFR, HER. Smiles: ON=C1C(=O)Nc2c1ccc(Cl)c2Cl. References: Stankevicius, Edgaras, Dalsgaard, Thomas, Kroigaard, Christel et al. Opening of small and intermediate calcium-activated potassium channels induces relaxation mainly mediated by nitric-oxide release in large arteries and endothelium-derived hyperpolarizin