219670
CFTR Inhibitor-172
≥95% (HPLC), solid, CFTR inhibitor, Calbiochem®
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CFTR Inhibitor-172, 3-[(3-Trifluoromethyl)phenyl]-5-[(4-carboxyphenyl)methylene]-2-thioxo-4-thiazolidinone, CFTR inh-172, 3-[(3-Trifluoromethyl)phenyl]-5-[(4-carboxyphenyl)methylene]-2-thioxo-4-thiazolidinone, CFTRinh-172
C18H10F3NO3S2
Recommended Products
Quality Level
Assay
≥95% (HPLC)
form
solid
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze
protect from light
color
yellow
solubility
DMSO: 5 mg/mL
shipped in
ambient
storage temp.
2-8°C
InChI
1S/C18H10F3NO3S2/c19-18(20,21)12-2-1-3-13(9-12)22-15(23)14(27-17(22)26)8-10-4-6-11(7-5-10)16(24)25/h1-9H,(H,24,25)/b14-8-
InChI key
JIMHYXZZCWVCMI-ZSOIEALJSA-N
General description
A cell-permeable 2-thio-4-thiazolidinone compound that acts as a potent, reversible, rapid, and voltage-independent inhibitor of CFTR (cystic fibrosis transmembrane conductance regulator)-mediated Cl- transport in human airway cells (Ki ~ 300 nM). It does not prevent elevation of cellular cAMP, nor does it inhibit non-CFTR Cl- channels, MDR-1, ATP-sensitive K+ channels, or a series of other transporters even at concentrations as high as 5 µM. Shown to block cholera toxin-induced intestinal fluid secretion in mice. May be also useful for reducing intestinal fluid loss in other secretory diarrheas.
A cell-permeable 2-thio-4-thiazolidinone compound that acts as a potent, reversible, rapid, and voltage-independent inhibitor of CFTR (cystic fibrosis transmembrane conductance regulator)-mediated Cl- transport in human airway cells (Ki ~ 300 nM). It does not prevent elevation of cellular cAMP, nor does it inhibit non-CFTR Cl- channels, MDR-1, ATP-sensitive K+ channels, or a series of other transporters even at concentrations as high as 5 µM. Shown to block cholera toxin-induced intestinal fluid secretion in mice. May be also useful for reducing intestinal fluid loss in other secretory diarrheas. Also available as a 50 mM solution in DMSO (Cat. No. 219674).
Biochem/physiol Actions
Cell permeable: yes
Primary Target
CFTR
CFTR
Product does not compete with ATP.
Reversible: yes
Target Ki: ~ 300 nM against CFTR (cystic fibrosis transmembrane conductance regulator)-mediated Cl- transport in human airway cells
Packaging
Packaged under inert gas
Warning
Toxicity: Standard Handling (A)
Reconstitution
Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Yang, H., et al. 2003. J. Biol. Chem.278, 35079.
Al-Awqati, Q., et al. 2002. J. Clin. Invest.110, 1599.
Ma, T., et al. 2002. J. Clin. Invest.110, 1651.
Al-Awqati, Q., et al. 2002. J. Clin. Invest.110, 1599.
Ma, T., et al. 2002. J. Clin. Invest.110, 1651.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
WGK
WGK 3
Certificates of Analysis (COA)
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Scientific reports, 11(1), 15511-15511 (2021-08-01)
The availability of a simple, robust and non-invasive in vitro airway model would be useful to study the functionality of the cystic fibrosis transmembrane regulator (CFTR) protein and to personalize modulator therapy for cystic fibrosis (CF) patients. Our aim was
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