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). It inhibits hyperpolarization of human, mouse, and rat erythrocytes induced by the calcium ionophore A23187 (Cay-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-gamma 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. 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.Formal Name: 4-[[3-(trifluoromethyl)phenyl]methyl]-2H-1,4-benzothiazin-3(4H)-one. CAS Number: 353262-04-1. Molecular Formula: C16H12F3NOS. Formula Weight: 323.3. Purity: >98%. Formulation: (Request formulation change), A crystalline solid. Solubility: DMF: 30 mg/ml, DMSO: 30 mg/ml, DMSO:PBS (pH 7.2) (1:1): 0.5 mg/ml, Ethanol: 20 mg/ml. lambdamax: 214, 239 nm. SMILES: O=C1N(CC2=CC=CC(C(F)(F)F)=C2)C3=CC=CC=C3SC1. InChi Code: InChI=1S/C16H12F3NOS/c17-16(18,19)12-5-3-4-11(8-12)9-20-13-6-1-2-7-14(13)22-10-15(20)21/h1-8H,9-10H2. InChi Key: ZUIJXKLTUFCDGO-UHFFFAOYSA-N.