CFTRinh 172
Chemical Name: 4-[[4-Oxo-2-thioxo-3-[3-trifluoromethyl)phenyl]-5-thiazolidinylidene]methyl]benzoic acid
Purity: ≥98%
Biological Activity
CFTRinh 172 is a voltage-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.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion.
Ma et al.
J.Clin.Invest., 2002;110:1651 -
Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blocker.
Taddei et al.
FEBS Lett., 2004;558:52 -
Small-molecule CFTR inhibitors slow cyst growth in polycystic kidney disease.
Yang et al.
J.Am.Soc.Nephrol., 2008;19:1300 -
Rescue of functional F508del cystic fibrosis transmembrane conductance regulator by vasoactive intestinal peptide in the human nasal epithelial cell line JME/CF15.
Rafferty et al.
J.Pharmacol.Exp.Ther., 2009;331:2 -
Cystic fibrosis transmembrane regulator inhibitors CFTRinh-172 and GlyH-101 target mitochondrial functions, independently of chloride channel inhibition.
Kelly et al.
J.Pharmaco.Exp.Ther., 2010;333:60
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Citations for CFTRinh 172
The citations listed below are publications that use Tocris products. Selected citations for CFTRinh 172 include:
5 Citations: Showing 1 - 5
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Esomeprazole Increases Airway Surface Liquid pH in Primary Cystic Fibrosis Epithelial Cells.
Authors: Delpiano Et al.
Front Pharmacol 2019;9:1462
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Cell volume changes contribute to epithelial morphogenesis in zebrafish Kupffer's vesicle.
Authors: Dasgupta Et al.
Elife 2018;7
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Signaling Cascade Involved in Rapid Stimulation of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by dexameth.
Authors: Bossmann Et al.
Int J Mol Sci 2017;18
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Glucocorticoids Distinctively Modulate the CFTR Channel with Possible Implications in Lung Development and Transition into Extrauterine Life.
Authors: Laube Et al.
PLoS One 2015;10:e0124833
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Benzimidazolones enhance the function of epithelial Na+ transport.
Authors: Laube Et al.
Br J Pharmacol 2013;168:1329
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