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General description
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）。
Biochem/physiol Actions
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
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%
Preparation Note
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。
Other Notes
Sonawane, N.D., et al. 2006.FASEB J.20, 130.
Muanprasat, C., et al. 2004.J. Gen.Physiol.124, 125.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
毒性：标准处理（A）
| Quality Level | 100 |
| assay | ≥97% (HPLC) |
| form | solid |
| manufacturer/tradename | Calbiochem® |
| storage condition | OK to freeze |
| color | yellow |
| solubility | DMSO: 200 mg/mL |
| shipped in | ambient |
| storage temp. | 2-8°C |
| SMILES string | 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 |
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¥ 1011.55
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¥ 521.16
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¥ 580.62
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¥ 1310.31
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¥ 1334.26
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¥ 2024.55
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¥ 381.67
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¥ 70526.15
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¥ 8072.66
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