In vitro activity: NS6180 is a novel potent and selective KCa3.1 channel inhibitor with IC50 of 9 nM. KCa3.1 channels are targets for pharmacological control of intestinal inflammation. NS6180 prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. NS6180 inhibited cloned human KCa3.1 channels via T250 and V275, the same amino acid residues conferring sensitivity to triarylmethanes such as like TRAM-34. NS6180 inhibited endogenously expressed KCa3.1 channels in human, mouse and rat erythrocytes, with similar potencies (15–20 nM).

Kinase Assay: NS6180 is a novel potent and selective KCa3.1 channel inhibitor with IC50 of 9 nM. KCa3.1 channels are targets for pharmacological control of intestinal inflammation.

Cell Assay: S6180 inhibited cloned human KCa3.1 channels via T250 and V275, the same amino acid residues conferring sensitivity to triarylmethanes such as like TRAM-34. NS6180 inhibited endogenously expressed KCa3.1 channels in human, mouse and rat erythrocytes, with similar potencies (15–20 nM).