NS6180

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

NS6180 是一种新型强效选择性 KCa3.1 通道抑制剂 (IC50= 9 nM)，可防止 T 细胞活化和炎症。

NS6180 is a novel potent and selective KCa3.1 channel inhibitor(IC50= 9 nM) prevents T-cell activation and inflammation.

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 (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).

NS6180 | NS-6180 | NS 6180

Cell Cycle/DNA Damage

Potassium Channel

KCa3.1 channel

Inflammation/Immunology

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353262-04-1

323.33

C16H12F3NOS

>98% (HPLC)

DMSO: 100 mM

O=C1CSC2=CC=CC=C2N1CC3=CC=CC(C(F)(F)F)=C3

4-[[3-(Trifluoromethyl)phenyl]methyl]-2H-1,4-benzothiazin-3(4H)-one

(-20℃)

With Ice Pack

≥ 2 years