NS 6180

NS 6180 is an inhibitor of the intermediate-conductance calcium-activated potassium channel 3.1 (IKCa1/KCa3.1; IC50 = 9.4 nM in HEK293 cells expressing the human channel).{43059} It inhibits hyperpolarization of human, mouse, and rat erythrocytes induced by the calcium ionophore A23187 (Item No. 11016) (IC50s = 14, 15, and 9 nM, respectively). NS 6180 is selective for IKCa1/KCa3.1 over voltage-gated sodium (Nav) and most voltage-gated potassium channels (Kv) but does inhibit KCa1.1, Kv1.3, and Kv11.1 channels by greater than 50% at 10 µM. It is selective for potassium channels over G protein-coupled receptors and ion channels, inhibiting only the norepinephrine and dopamine transporters, L-type calcium channel, and melatonin receptor MT1 by greater than 50% in a panel of 69 receptors and channels. NS 6180 inhibits T-lymphocyte activation and the release of the Th1 cytokines IL-2 and IFN-? in vitro (IC50 = ~50 nM). It also increases proliferation of natural killer (NK) cells and selectively increases cytotoxicity of adherent, but not non-adherent, NK cells.{43560} In a rat model of inflammatory bowel disease (IBD) induced by DNBS, NS 6180 (3 and 10 mg/kg per day) decreases colon inflammation and improves weight gain.{43059}