| 货号 | 15545-50mg |
| 描述 | The cystic fibrosis (CF) gene encodes a cAMP-regulated chloride channel, the CF transmembrane conductance regulator (CFTR).1 CFTR Inhibitor-172 is a thiazolidinone that selectively blocks the CFTR channel (Ki = 300 nM) in a voltage-independent manner.2 It appears to directly modulate the gating of chloride at the channel and does not prevent elevation of cAMP or inhibit other pumps or channels.2,3 In mice, CFTR inhibitor-172 prevents cholera toxin-induced fluid secretion in the small intestine, when given by intraperitoneal injection.2,4 It slows cyst growth in animal models of polycystic kidney disease.5 As CFTR also modulates glutathione (GSH) efflux, CFTR inhibitor-172 can affect intracellular GSH concentration and reactive oxygen species balance.6,7,8 |
| 别名 | CFTR(inh)-172;Cystic Fibrosis Transmembrane Conductance Regulator Inhibitor 172; |
| 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.Ma, T.,Thiagarajah, J.R.,Yang, H., et al. Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. Journal of Clinical Investigation 110(11), 1651-1658 (2002). 3.Taddei, A.,Folli, C.,Zegarra-Moran, O., et al. Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blocker. FEBS Letters 558(1-3), 52-56 (2004). 4.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). 5.Yang, B.,Sonawane, N.D.,Zhao, D., et al. Small-molecule CFTR inhibitors slow cyst growth in polycystic kidney disease. Journal of the American Society of Nephrology 19(7), 1300-1310 (2008). 6.Duranton, C.,Rubera, I.,Cougnon, M., et al. CFTR is involved in the fine tuning of intracellular redox status: Physiological implications in cystic fibrosis. American Journal of Pathology 181(4), 1367-1377 (2012). 7.lHoste, S.,Chargui, A.,Belfodil, R., et al. CFTR mediates apoptotic volume decrease and cell death by controlling glutathione efflux and ROS production in cultured mice proximal tubules. American Journal of Physiology.Renal Physiology 298(2), F435-F453 (2010). 8.Rubera, I.,Duranton, C.,Melis, N., et al. Role of CFTR in oxidative stress and suicidal death of renal cells during cisplatin-induced nephrotoxicity. Cell Death Dis. 4, 1-10 (2013). | |
| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥98% |
| 计算分子量 | 409.4 |
| 分子式 | C18H10F3NO3S2 |
| CAS号 | 307510-92-5 |
| 稳定性 | ≥ 2 years |
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