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Description: 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).
References: Br J Pharmacol. 2013 Jan; 168(2):432-44.
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