推荐产品
product name
CFTR抑制剂II,GlyH-101, CFTR Inhibitor II, GlyH-101, CAS 328541-79-3, is a cell-permeable potent, selective and reversible open-channel blocker of CFTR (Ki = 4.3 µM in CFTR-expressing FRT cells).
质量水平
检测方案
≥97% (HPLC)
形式
solid
制造商/商品名称
Calbiochem®
储存条件
OK to freeze
颜色
yellow
溶解性
DMSO: 200 mg/mL
运输
ambient
储存温度
2-8°C
InChI
1S/C19H15Br2N3O3/c20-15-8-13(18(26)17(21)19(15)27)9-23-24-16(25)10-22-14-6-5-11-3-1-2-4-12(11)7-14/h1-9,22,26-27H,10H2,(H,24,25)/b23-9+
InChI key
RMBDLOATEPYBSI-NUGSKGIGSA-N
一般描述
一种可渗透细胞的甘氨酰腙化合物,以中等速度作为CFTR的有效,选择性和可逆的开放通道阻滞剂(<1 min; 95% inhibition at 50 µM; Ki = 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl- current) and exhibits desirable aqueous solubility. Shown to produce inwardly rectifying CFTR Cl- currents with reduced mean channel open time and suggested to directly interact with the channel pore at the extracellular side of the membrane. Displays minimal effects on P-glycoprotein and non-CFTR-mediated Cl- currents, and is effective in nasal and intestinal epithelia in vivo. Also available as a 25 mM solution in DMSO (Cat. No. 219675)。
一种可渗透细胞的甘氨酰腙化合物,可作为CFTR的有效,选择性和可逆的开放通道阻滞剂,具有中等速度(<1 min;在50 µM时抑制95%;Ki = 4.3 µM,在表达CFTR的FRT细胞中用于顶膜Cl- 电流),并表现出理想的水溶性。已显示可产生向内整流的CFTR Cl-电流,且平均通道开放时间减少,并建议与膜细胞外侧的通道孔直接相互作用。显示对P-糖蛋白和非CFTR介导的Cl-电流的影响最小,并且在体内对鼻和肠上皮有效。
生化/生理作用
在表达CFTR的FRT细胞中为4.3 µM,用于顶膜氯离子电流
主要靶标
CFTR
CFTR
产物不与ATP竞争。
可逆性:是
细胞可渗透性:是
靶标IC50:以50 µM时抑制95%
警告
毒性:标准处理(A)
重悬
复溶后,等分并冷冻保存(-20°C)。储备液在-20°C条件下可稳定保存3个月。
其他说明
Sonawane, N.D., et al. 2006.FASEB J.20, 130.
Muanprasat, C., et al. 2004.J. Gen.Physiol.124, 125.
Muanprasat, C., et al. 2004.J. Gen.Physiol.124, 125.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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