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 (EC₅₀

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 (EC₅₀ = 1.6μM in CFTR-expressing Fisher rat thyroid cells). Also shown to activate δF508-CFTR in primary CF-HBE cell cultures (EC₅₀ = 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 Ca²⁺-activated Cl^- channel (TMEM16A) or intracellular Ca²⁺ levels.

Specifications

• Color: Light Yellow
• Description: 98% by HPLC
• Target Proteins: CFTR
• Molecular Formula: C₁₆H₁₃N₅O
• Solubility: DMSO
• Content And Storage: Protect from light
• Form: Powder
• Quantity: 10 mg