MilliporeSigma™ Calbiochem™ CFTR Activator, Cact-A1

Description

• A cell-permeable, non-toxic aminopyrazolocarbonitrile compound that acts as a potent, selective, reversible and cAMP-independent activator of CFTR-dependent Cl - channel in airway epithelial cells (EC 50 = 1.6μM in CFTR-expressing Fisher rat thyroid cells)
• Also shown to activate δF508-CFTR in primary CF-HBE cell cultures (EC 50 = 3.5μM)
• Reported to directly bind to the same site as CFTR inh -172 ( Cat
• No
• 219670, Cat
• No
• 219674)
• Does neither elevate intracellular cAMP levels nor appear to have any requirement for cAMP agonist, such as forskolin (Cat
• No
• 344270, Cat
• No
• 344282)
• Shown to additively potentiate the G551D-CFTR Cl - current activated by forskolin with CFTR potentiator, VX-770
• Exerts no effect on either Ca 2+ -activated Cl - channel (TMEM16A) or intracellular Ca 2+ levels.