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Submit ReviewCFTRinh 172
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)
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 |
| InChI Key | JIMHYXZZCWVCMI-RIYZIHGNSA-N |
| 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 | |
|---|---|---|---|
| Solubility | |||
| 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.
| 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
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:
Richard C et al (2020) The odorant receptor OR2W3 on airway smooth muscle evokes bronchodilation via a cooperative chemosensory tradeoff between TMEM16A and CFTR. Proc Natl Acad Sci U S A 117 28485-28495 PMID: 33097666
Michael A et al (2020) 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. Cells 9 PMID: 32967385
Jason P et al (2020) Osmotic Gradients in Epithelial Acini Increase Mechanical Tension across E-cadherin, Drive Morphogenesis, and Maintain Homeostasis. Curr Biol 30 624-633.e4 PMID: 31983640
Rayner et al (2019) Mechanism and effects of pulsatile GABA secretion from cytosolic pools in the human beta cell. Nat Metab 1 1110-1126 PMID: 32432213
Dasgupta et al (2018) Cell volume changes contribute to epithelial morphogenesis in zebrafish Kupffer's vesicle. Elife 7 PMID: 29376824
Laube et al (2015) Glucocorticoids Distinctively Modulate the CFTR Channel with Possible Implications in Lung Development and Transition into Extrauterine Life. PLoS One 10 e0124833 PMID: 25910246
Delpiano et al (2019) Esomeprazole Increases Airway Surface Liquid pH in Primary Cystic Fibrosis Epithelial Cells. Front Pharmacol 9 1462 PMID: 30618754
Bossmann et al (2017) Signaling Cascade Involved in Rapid Stimulation of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by dexameth. Int J Mol Sci 18 PMID: 28825630
Laube et al (2013) Benzimidazolones enhance the function of epithelial Na+ transport. Br J Pharmacol 168 1329 PMID: 23083067
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
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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