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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
5 Citations for CFTRinh 172
Citations are publications that use Tocris products. Selected citations for CFTRinh 172 include:
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
Delpiano et al (2019) Esomeprazole Increases Airway Surface Liquid pH in Primary Cystic Fibrosis Epithelial Cells. Front Pharmacol 9 1462 PMID: 30618754
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
Dasgupta et al (2018) Cell volume changes contribute to epithelial morphogenesis in zebrafish Kupffer's vesicle. Elife 7 PMID: 29376824
Do you know of a great paper that uses CFTRinh 172 from Tocris? Please let us know.
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Ion Channel Product Listing
A collection of around 500 products for ion channel research, the listing includes research tools for the study of:
- Ligand-gated ion channels
- Voltage-gated ion channels
- Other Ion Channels