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CAS No. : 353262-04-1
MCE 国际站:NS6180
产品活性:NS6180 是一种新型的 KCa3.1 通道抑制剂,具有口服活性。NS6180 对克隆的人KCa3.1 通道具有抑制作用,其 IC50 值为 9 nM。NS6180 可用于炎症性肠病 (IBD) 的研究。
研究领域:Membrane Transporter/Ion Channel
作用靶点:Potassium Channel
In Vitro: NS6180 (0.001-1 μM) shows inhibition of human KCa3.1 with an IC50 value of 9.4 nM and a K50 value of 11 1.7 nM, respectively.
NS6180 (30 nM, 10 μM) has inhibition that dependent on amino acid residues T250 and V275.
NS6180 (1, 10, 100 and 1000 nM; 1 min) shows CCCPreported hyperpolarizations of human erythrocytes.
NS6180 (1, 10, 100 and 1000 nM; 1 min) blocks the erythrocyte KCa3.1 channels with IC50 values of 14 nM (human KCa3.1 channels), 15 nM (mouse) and 9 nM (rats), respectively.NS6180 (0-5 μM, 48 h) suppresses rat and mouse splenocyte proliferation at submicrolar concentrations and potently inhibited IL-2 and IFN-g production, while exerting smaller effects on IL-4 and TNF-α and no effect on IL-17 production.
In Vivo: NS6180 (i.v., i.p. and oral administration; 10 mg/kg; twice daily or once daily) has extremely low bioavailability and reduces DNBS-induced experimental colitis in rats.
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