An inhibitor of IKCa1/KCa3.1 channels (IC50 = 9.4 nM); inhibits A23187-induced hyperpolarization of human

NS 6180 – 10 mg

Brand:
Cayman
CAS:
353262-04-1
Storage:
-20
UN-No:
Non-Hazardous - /

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).{43059} 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/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-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.{43560} 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.{43059}  

 

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Description

An inhibitor of IKCa1/KCa3.1 channels (IC50 = 9.4 nM); inhibits A23187-induced hyperpolarization of human, mouse, and rat erythrocytes (IC50s = 14, 15, and 9 nM, respectively); selective over Nav and most Kv channels as well as 65 receptors and channels in a panel; inhibits T-lymphocyte activation and cytokine release in vitro (IC50 = ~50 nM); decreases colon inflammation and improves weight gain in a rat model of DNBS-induced IBD

Formal name: 4-[[3-(trifluoromethyl)phenyl]methyl]-2H-1,4-benzothiazin-3(4H)-one

Synonyms: 

Molecular weight: 323.3

CAS: 353262-04-1

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Ion Channel Modulation|Blockers||Research Area|Immunology & Inflammation|Adaptive Immunity||Research Area|Immunology & Inflammation|Gastric Disease|Ulcerative Colitis||Research Area|Immunology & Inflammation|Innate Immunity

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