CFTRinh 172

Catalog # Availability Size / Price Qty
3430/10
3430/50
CFTRinh 172 | CAS No. 307510-92-5 | CFTR Blockers
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Description: Voltage-independent, selective CFTR chloride channel blocker

Chemical Name: 4-[[4-Oxo-2-thioxo-3-[3-trifluoromethyl)phenyl]-5-thiazolidinylidene]methyl]benzoic acid

Purity: ≥98%

Product Details
Citations (12)
Reviews

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

M.Wt:
409.4
Formula:
C18H10F3NO3S2
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at +4°C
CAS No:
307510-92-5

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

  1. A xenogeneic-free system generating functional human gut organoids from pluripotent stem cells
    H Uchida, M Machida, T Miura, T Kawasaki, T Okazaki, K Sasaki, S Sakamoto, N Ohuchi, M Kasahara, A Umezawa, H Akutsu
    JCI Insight, 2017;2(1):e86492.
  2. Disabled-2 protein facilitates assembly polypeptide-2-independent recruitment of cystic fibrosis transmembrane conductance regulator to endocytic vesicles in polarized human airway epithelial cells.
    Cihil KM, Ellinger P, Fellows A, Stolz DB, Madden DR, Swiatecka-Urban A
    J. Biol. Chem., 2012;287(18):15087-99.
  3. Thiazolidinone CFTR inhibitor identified by high-throughput screening blocks cholera toxin-induced intestinal fluid secretion.
    Ma et al.
    J.Clin.Invest., 2002;110:1651
  4. Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blocker.
    Taddei et al.
    FEBS Lett., 2004;558:52
  5. Small-molecule CFTR inhibitors slow cyst growth in polycystic kidney disease.
    Yang et al.
    J.Am.Soc.Nephrol., 2008;19:1300
  6. 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
  7. 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:

12 Citations: Showing 1 - 10

  1. Clinical and molecular characterization of the R751L-CFTR mutation.
    Authors: Ineke Et al.
    Am J Physiol Lung Cell Mol Physiol  2021;320:L288-L300
  2. Epidermal growth factor strongly affects epithelial Na+ transport and barrier function in fetal alveolar cells, with minor sex-specific effects.
    Authors: Mandy Et al.
    Sci Rep  2021;11:15951
  3. Choice of Differentiation Media Significantly Impacts Cell Lineage and Response to CFTR Modulators in Fully Differentiated Primary Cultures of Cystic Fibrosis Human Airway Epithelial Cells.
    Authors: Michael A Et al.
    Cells  2020;9
  4. Osmotic Gradients in Epithelial Acini Increase Mechanical Tension across E-cadherin, Drive Morphogenesis, and Maintain Homeostasis.
    Authors: Jason P Et al.
    Curr Biol  2020;30:624-633.e4
  5. The odorant receptor OR2W3 on airway smooth muscle evokes bronchodilation via a cooperative chemosensory tradeoff between TMEM16A and CFTR.
    Authors: Richard C Et al.
    Proc Natl Acad Sci U S A  2020;117:28485-28495
  6. Esomeprazole Increases Airway Surface Liquid pH in Primary Cystic Fibrosis Epithelial Cells.
    Authors: Delpiano Et al.
    Front Pharmacol  2019;9:1462
  7. Mechanism and effects of pulsatile GABA secretion from cytosolic pools in the human beta cell.
    Authors: Rayner Et al.
    Nat Metab  2019;1:1110-1126
  8. Cell volume changes contribute to epithelial morphogenesis in zebrafish Kupffer's vesicle.
    Authors: Dasgupta Et al.
    Elife  2018;7
  9. 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
  10. 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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