Cat. No. 3430
Chemical Name: 4-[[4-Oxo-2-thioxo-3-[3-trifluorome
Biological ActivityVoltage-independent, selective CFTR chloride channel blocker (Ki = 300 nM) that alters channel gating. Blocks intestinal fluid secretion induced by cholera toxin and Escherichia coli and suppresses cyst growth in animal models of polycystic kidney disease. Orally active. Inhibits mitochondrial respiration and increases reactive oxygen species (ROS) production independently of CFTR in several cell lines.
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
All Tocris products are intended for laboratory research use only.
Certificate of Analysis / Safety Data Sheet
Kelly et al (2010) Cystic fibrosis transmembrane regulator inhibitors CFTRinh-172 and GlyH-101 target mitochondrial functions, independently of chloride channel inhibition. J.Pharmaco.Exp.Ther. 333 60.
Rafferty et al (2009) Rescue of functional F508del cystic fibrosis transmembrane conductance regulator by vasoactive intestinal peptide in the human nasal epithelial cell line JME/CF15. J.Pharmacol.Exp.Ther. 331 2. PMID: 19584307.
Yang et al (2008) Small-molecule CFTR inhibitors slow cyst growth in polycystic kidney disease. J.Am.Soc.Nephrol. 19 1300. PMID: 18385427.
Taddei et al (2004) Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blocker. FEBS Lett. 558 52. PMID: 14759515.
Ma et al (2002) Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion. J.Clin.Invest. 110 1651. PMID: 12464670.
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Citations are publications that use Tocris products. Selected citations for CFTRinh 172 include:
Laube et al (2015) Glucocorticoids Distinctively Modulate the CFTR Channel with Possible Implications in Lung Development and Transition into Extrauterine Life. PLoS One 10 e0124833. PMID: 25910246.
Laube et al (2013) Benzimidazolones enhance the function of epithelial Na+ transport. Br J Pharmacol 168 1329. PMID: 23083067.
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Keywords: CFTRinh 172, supplier, Voltage-independent, selective, CFTR, chloride, channel, blockers, Cl-, Channels, CFTRinh172, Tocris Bioscience, Chloride Channel Blocker products