推荐产品
产品名称
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
方案
≥97% (HPLC)
表单
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
SMILES字符串
Brc1c(c(cc(c1O)\C=N\NC(=O)CNc2cc3c(cc2)cccc3)Br)O
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
储存分类代码
11 - Combustible Solids
WGK
WGK 2
闪点(°F)
Not applicable
闪点(°C)
Not applicable
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