Biochem/physiol Actions

Reversible: yes

Product does not compete with ATP.

Target IC₅₀: 95% inhibition at 50 µM

Primary TargetCFTR

Cell permeable: yes

Target K_i: 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl- current

General description

A cell-permeable glycinyl hydrazone compound that acts as a potent, selective and reversible open-channel blocker of CFTR with intermediate speed (﹤1 min; 95% inhibition at 50 µM; K_i = 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl^- current) and exhibits desirable aqueous solubility. Shown to produce inwardly rectifying CFTR Cl^- currents with reduced mean channel open time and suggested to directly interact with the channel pore at the extracellular side of the membrane. Displays minimal effects on P-glycoprotein and non-CFTR-mediated Cl^- currents, and is effective in nasal and intestinal epithelia in vivo.

A cell-permeable glycinyl hydrazone compound that acts as a potent, selective and reversible open-channel blocker of CFTR with intermediate speed (﹤1 min; 95% inhibition at 50 µM; K_i = 4.3 µM in CFTR-expressing FRT cells for apical membrane Cl^- current) and exhibits desirable aqueous solubility. Shown to produce inwardly rectifying CFTR Cl^- currents with reduced mean channel open time and suggested to directly interact with the channel pore at the extracellular side of the membrane. Displays minimal effects on P-glycoprotein and non-CFTR-mediated Cl^- currents, and is effective in nasal and intestinal epithelia in vivo. Also available as a 25 mM solution in DMSO (Cat. No. 219675).

Legal Information

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

Other Notes

Sonawane, N.D., et al. 2006. FASEB J.20, 130.Muanprasat, C., et al. 2004. J. Gen. Physiol.124, 125.

Packaging

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)