CFTRinh 172

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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% (HPLC)
Citations (12)

Biological Activity for CFTRinh 172

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 for CFTRinh 172

M. Wt 409.4
Formula C18H10F3NO3S2
Storage Store at +4°C
Purity ≥98% (HPLC)
CAS Number 307510-92-5
PubChem ID 1554210
Smiles O=C(N(C3=CC=CC(C(F)(F)F)=C3)C(S2)=S)\C2=C/C1=CC=C(C(O)=O)C=C1

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.

Solubility Data for CFTRinh 172

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 40.94 100

Preparing Stock Solutions for CFTRinh 172

The following data is based on the product molecular weight 409.4. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.44 mL 12.21 mL 24.43 mL
5 mM 0.49 mL 2.44 mL 4.89 mL
10 mM 0.24 mL 1.22 mL 2.44 mL
50 mM 0.05 mL 0.24 mL 0.49 mL

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Product Datasheets for CFTRinh 172

Certificate of Analysis / Product Datasheet
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References for CFTRinh 172

References are publications that support the biological activity of the product.

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

Taddei et al (2004) Altered channel gating mechanism for CFTR inhibition by a high-affinity thiazolidinone blocker. FEBS Lett. 558 52 PMID: 14759515

Yang et al (2008) Small-molecule CFTR inhibitors slow cyst growth in polycystic kidney disease. J.Am.Soc.Nephrol. 19 1300 PMID: 18385427

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

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

If you know of a relevant reference for CFTRinh 172, please let us know.

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Keywords: CFTRinh 172, CFTRinh 172 supplier, Voltage-independent, selective, CFTR, chloride, channel, blockers, Cl-, Channels, CFTRinh172, 3430, Tocris Bioscience

12 Citations for CFTRinh 172

Citations are publications that use Tocris products. Selected citations for CFTRinh 172 include:

Ineke et al (2021) Clinical and molecular characterization of the R751L-CFTR mutation. Am J Physiol Lung Cell Mol Physiol 320 L288-L300 PMID: 33296276

Mandy et al (2021) Epidermal growth factor strongly affects epithelial Na+ transport and barrier function in fetal alveolar cells, with minor sex-specific effects. Sci Rep 11 15951 PMID: 34354180

Laube et al (2013) Benzimidazolones enhance the function of epithelial Na+ transport. Br J Pharmacol 168 1329 PMID: 23083067

Agnieszka et al (2013) c-Cbl reduces stability of rescued ?F508-CFTR in human airway epithelial cells: Implications for cystic fibrosis treatment. Commun Integr Biol 6 e23094 PMID: 23750297

Do you know of a great paper that uses CFTRinh 172 from Tocris? Please let us know.

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