Biochem/physiol Actions

Reversible: yes

Primary TargetCFTR ion-channel

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. The solid form of this compound (Cat. No. 219670) is also available.

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

5 mg in Glass bottle

Packaged under inert gas

Physical form

A 50 mM (5 mg/244 µL) solution of CFTR Inhibitor-172 (Cat. No. 219670) in DMSO.

Reconstitution

Following initial thaw, aliquot and freeze (70°C). Aliquots are stable for up to 3 months at -70°C.

Warning

Toxicity: Irritant (B)