Biochem/physiol Actions

Reversible: yes

Product does not compete with ATP.

Primary TargetCFTR

Target K_i: ~ 300 nM against CFTR (cystic fibrosis transmembrane conductance regulator)-mediated Cl- transport in human airway cells

Cell permeable: yes

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 (K_i ~ 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).

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 (K_i ~ 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.

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

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.

Packaging

Packaged under inert gas

5 mg in Plastic ampoule

Reconstitution

Following reconstitution aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Warning

Toxicity: Standard Handling (A)