产品
编 号：F333241
分子式：C16H12F3NOS
分子量：323.33
分子式：C16H12F3NOS
分子量：323.33
产品类型
规格
价格
是否有货
10mM*1mL in DMSO
询价
询价
5mg
520
In-stock
10mg
880
In-stock
50mg
3280
In-stock
结构图
CAS No: 353262-04-1
产品详情
生物活性：
NS6180 is a new orally active KCa3.1 channel inhibitor. NS6180 inhibits cloned human KCa3.1 channels with an IC50value of 9 nM. NS6180 can be used for the research of inflammatory bowel disease (IBD) .
体内研究：
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.Animal Model:Rats
Dosage:10 mg/kg
Administration:i.v., i.p. and oral administration; 10 mg/kg; twice daily or once daily
Result:Had a plasma half-life of 3.8 h, oral or i.p. administration gave low plasma exposure (Cmax: 186 nM and 33 nM, respectively, after administration of 10 mg/kg).
体外研究：
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 CCCPreportedhyperpolarizations 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 andTNF-α and no effect on IL-17 production.
NS6180 is a new orally active KCa3.1 channel inhibitor. NS6180 inhibits cloned human KCa3.1 channels with an IC50value of 9 nM. NS6180 can be used for the research of inflammatory bowel disease (IBD) .
体内研究：
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.Animal Model:Rats
Dosage:10 mg/kg
Administration:i.v., i.p. and oral administration; 10 mg/kg; twice daily or once daily
Result:Had a plasma half-life of 3.8 h, oral or i.p. administration gave low plasma exposure (Cmax: 186 nM and 33 nM, respectively, after administration of 10 mg/kg).
体外研究：
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 CCCPreportedhyperpolarizations 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 andTNF-α and no effect on IL-17 production.
产品资料
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