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.
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All Tocris products are intended for laboratory research use only.
Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion.
Ma et al.
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.
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.
Cystic fibrosis transmembrane regulator inhibitors CFTRinh-172 and GlyH-101 target mitochondrial functions, independently of chloride channel inhibition.
Kelly et al.
The citations listed below are publications that use Tocris products. Selected citations for CFTRinh 172 include:
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