NS 6180

NS 6180 is an inhibitor of the intermediate-conductance calcium-activated potassium channel 3.1 (IKCa1/K_Ca3.1; IC₅₀ = 9.4 nM in HEK293 cells expressing the human channel).¹ 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/K_Ca3.1 over voltage-gated sodium (Na_v) and most voltage-gated potassium channels (K_v) but does inhibit K_Ca1.1, K_v1.3, and K_v11.1 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-γ 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.² 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.¹

WARNING This product is not for human or veterinary use.

1. Strøbæk, D., Brown, D.T., Jenkins, D.P., et al. NS6180, a new KCa 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. Br. J. Pharmacol. 168(2), 432-444 (2013).

2. Parzych, K.R., and Klionsky, D.J. An overview of autophagy: Morphology, mechanism, and regulation. Antioxid. Redox Signal. 20(3), 460-473 (2014).