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).
品質等級
化驗
≥97% (HPLC)
形狀
solid
製造商／商標名
Calbiochem®
儲存條件
OK to freeze
顏色
yellow
溶解度
DMSO: 200 mg/mL
運輸包裝
ambient
儲存溫度
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 密鑰
RMBDLOATEPYBSI-NUGSKGIGSA-N
一般說明
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）
重構
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。
其他說明
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.
法律資訊
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
儲存類別代碼
11 - Combustible Solids
水污染物質分類（WGK）
WGK 2
閃點（°F）
Not applicable
閃點（°C）
Not applicable
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