| 货号 | 15772-1mg |
| 描述 | The cystic fibrosis (CF) gene encodes a cAMP-regulated chloride channel, the CF transmembrane conductance regulator (CFTR).1 CFTR inhibitor II, also known as GlyH-101, is a glycine hydrazide that selectively and reversibly blocks the CFTR channel (Ki = 4.3 µM).2,3 This compound binds to a site at the external pore of CFTR, occluding the pore and rapidly preventing chloride transport.2,3 Intraluminal CFTR inhibitor II greatly reduces intestinal fluid secretion induced by cholera toxin.3 It is effective in cells in culture and also in nasal and intestinal epithelia in vivo.4,5,6,7 |
| 别名 | GlyH-101;Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor II; |
| 供应商 | Cayman |
| 应用文献 | |
| 1.Derand, R.,Bulteau-Pignoux, L. and Becq, F. The cystic fibrosis mutation G551D alters the non-Michaelis-Menten behavior of the cystic fibrosis transmembrane conductance regulator (CFTR) channel and abolishes the inhibitory genistein binding site. The Journal of Biological Chemisty 277(39), 35999-36004 (2002). 2.Sonawane, N.D.,Hu, J.,Muanprasat, C., et al. Luminally active, nonabsorbable CFTR inhibitors as potential therapy to reduce intestinal fluid loss in cholera. The FASEB Journal 20(1), 130-132 (2006). 3.Muanprasat, C.,Sonawane, N.D.,Salinas, D., et al. Discovery of glycine hydrazide pore-occluding CFTR inhibitors: Mechanism, structure-activity analysis, and in vivo efficacy. Journal of General Physiology 124(2), 125-137 (2004). 4.MacVinish, L.J.,Cope, G.,Ropenga, A., et al. Chloride transporting capability of Calu-3 epithelia following persistent knockdown of the cystic fibrosis transmembrane conductance regulator, CFTR. British Journal of Pharmacology 150(8), 1055-1065 (2007). 5.Garnett, J.P.,Hickman, E.,Tunkamnerdthai, O., et al. Protein phosphatase 1 coordinates CFTR-dependent airway epithelial HCO3- secretion by reciprocal regulation of apical and basolateral membrane Cl--HCO3- exchangers. British Journal of Pharmacology 168(8), 1946-1960 (2013). 6.Schiffhauer, E.S.,Vij, N.,Kovbasnjuk, O., et al. Dual activation of CFTR and CLCN2 by lubiprostone in murine nasal epithelia. American Journal of Physiology.Lung Cellular and Molecular Physiology 304(5), L324-L331 (2013). 7.Zertal-Zidani, S.,Busiah, K.,Edelman, A., et al. Small-molecule inhibitors of the cystic fibrosis transmembrane conductance regulator increase pancreatic endocrine cell development in rat and mouse. Diabetologia 56(2), 330-339 (2013). | |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 493.2 |
| 分子式 | C19H15Br2N3O3 |
| CAS号 | 328541-79-3 |
| 稳定性 | ≥ 2 years |
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