CFTRinh 172

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Cat.No. 3430 - CFTRinh 172 | C18H10F3NO3S2 | CAS No. 307510-92-5
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)
Datasheet
Citations (3)
Reviews
Literature

Biological 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.

Compound Libraries

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Technical Data

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.

All Tocris products are intended for laboratory research use only.

Solubility Data

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

Preparing Stock Solutions

The following data is based on the product molecular weight 409.4. Batch specific molecular weights may vary from batch to batch due to solvent 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

Certificate of Analysis / Product Datasheet
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Safety Datasheet

References

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


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

3 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 Dexamethasone. 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

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


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Literature in this Area

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