CFTR(inh)-172

Catalog #:

IN0044

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IN0044-5mg

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Synonyms: CFTR(inh)-172

IUPAC Name:

4-[[4-Oxo-2-thioxo-3-[3-trifluorome thyl)phenyl]-5-thiazolidinylidene]methyl]benzoic acid

Functional Activity:

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 in 100 mM DMSO

Purity: >97%

Storage: Store at 4 °C

CAS No.: 307510-92-5

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References for CFTR(inh)-172:

1. Kelly, M., Trudel, S., Brouillard, F., Bouillaud, F., Colas, J., Nguyen-Khoa, T., Ollero, M., Edelman, A., and Fritsch, J. Cystic fibrosis transmembrane regulator inhibitors CFTR(inh)-172 and GlyH-101 target mitochondrial functions, independently of chloride channel inhibition. J Pharmacol Exp Ther, 333: 60-69.

2. Caci, E., Caputo, A., Hinzpeter, A., Arous, N., Fanen, P., Sonawane, N., Verkman, A. S., Ravazzolo, R., Zegarra-Moran, O., and Galietta, L. J. Evidence for direct CFTR inhibition by CFTR(inh)-172 based on Arg347 mutagenesis. Biochem J, 413: 135-142, 2008.

3. Yang, B., Sonawane, N. D., Zhao, D., Somlo, S., and Verkman, A. S. Small-molecule CFTR inhibitors slow cyst growth in polycystic kidney disease. J Am Soc Nephrol, 19: 1300-1310, 2008.

Certificate of Analysis/MSDS is available upon request with lot number