Biochem/physiol Actions

Reversible: yes

Cell permeable: yes

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.

Legal Information

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

Packaging

5 mg in Glass bottle

Packaged under inert gas

Physical form

A 25 mM (5 mg/406 µL) solution of CFTR Inhibitor II, GlyH-101 (Cat. No. 219671) 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)