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; Ki = 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.
Biochem/physiol Actions
Cell permeable: yes
Reversible: yes
Packaging
Packaged under inert gas
Warning
Toxicity: Irritant (B)
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.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
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- UPC:
- 51171608
- Condition:
- New
- Availability:
- 3-5 Days
- Weight:
- 1.00 Ounces
- HazmatClass:
- No
- MPN:
- 219675-5MG
- CAS:
- 328541-79-3
- Temperature Control Device:
- Yes