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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.
This website uses cookies, which are necessary for the technical operation of the website and are always set. Other cookies, which increase the usability of this website, serve for direct advertising or simplify interaction with other websites and social networks, will only be used with your consent.
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