NS6180

NS6180 is a new orally active KCa3.1 channel inhibitor. NS6180 inhibits cloned human KCa3.1 channels with an IC₅₀value of 9 nM. NS6180 can be used for the research of inflammatory bowel disease (IBD) ^[1]. In Vitro: NS6180 (0.001-1 μM) shows inhibition of human KCa3.1 with an IC₅₀ value of 9.4 nM and a K₅₀ value of 11 1.7 nM, respectively^[1].
NS6180 (30 nM, 10 μM) has inhibition that dependent on amino acid residues T250 and V275^[1].
NS6180 (1, 10, 100 and 1000 nM; 1 min) shows CCCPreported hyperpolarizations of human erythrocytes^[1].
NS6180 (1, 10, 100 and 1000 nM; 1 min) blocks the erythrocyte KCa3.1 channels with IC₅₀ values of 14 nM (human KCa3.1 channels), 15 nM (mouse) and 9 nM (rats), respectively^[1]. NS6180 (0-5 μM, 48 h) suppresses rat and mouse splenocyte proliferation at submicrolar concentrations and potently inhibited IL-2 and IFN-g production, while exerting smaller effects on IL-4 and TNF-α and no effect on IL-17 production^[1].
In Vivo: NS6180 (i.v., i.p. and oral administration; 10 mg/kg; twice daily or once daily) has extremely low bioavailability and reduces DNBS-induced experimental colitis in rats^[1].