貨號	規格	價格	上海	北京	武漢	南京
S85054-5mg	98.0%	￥200.00 S85054-5mg ￥200.00 現貨	10 10	-	-	-
S85054-10mg	98.0%	￥300.00 S85054-10mg ￥300.00 現貨	9 9	-	-	-
S85054-25mg	98.0%	￥680.00 S85054-25mg ￥680.00 現貨	6 6	-	-	-
S85054-50mg	98.0%	￥1011.50 S85054-50mg ￥1011.50 現貨	5 5	-	-	-
S85054-100mg	98.0%	￥1530.00 S85054-100mg ￥1530.00 現貨	5 5	-	-	-

產品介紹

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)

產品描述：

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)

靶點：

Potassium Channel;PotassiumChannel

體外研究：

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 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

體內研究：

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).

參考文獻：

1. Strobak D, et al. NS6180, a new K(Ca) 3.1 channel inhibitor prevents T-cell activation and inflammation in a rat model of inflammatory bowel disease. Br J Pharmacol. 2013 Jan;168(2):432-44.

溶解性：

Soluble in DMSO

保存條件：

-20℃

配置溶液濃度參考：

	1mg	5mg	10mg
1 mM	3.093 ml	15.464 ml	30.928 ml
5 mM	0.619 ml	3.093 ml	6.186 ml
10 mM	0.309 ml	1.546 ml	3.093 ml
50 mM	0.062 ml	0.309 ml	0.619 ml

注意：

部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。

參考文獻

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