CFTR Activator, Cact-A1

Biochemicals / Biochem-Agonists

4°C

Supplied as a light yellow powder.

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 = 1.6uM in CFTR-expressing Fisher rat thyroid cells). Also shown to activate deltaF508-CFTR in primary CF-HBE cell cultures (EC50 = 3.5uM). Reported to directly bind to the same site as CFTRinh-172. Does neither elevate intracellular cAMP levels nor appear to have any requirement for cAMP agonist, such as forskolin. 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.

Synonyms:
Cystic Fibrosis Transmembrane Conductance Regulator Activator, Cact-A1, 5-((Z)-2-(2-(Allyloxy)phenyl)-1-cyanovinyl)-3-amino-1H-pyrazole-4-carbonitrile, (Z)-3-(2-(2-(Allyloxy)phenyl)-1-cyanovinyl)-5-amino-1H-pyrazole-4-carbonitrile

Molecular Formula:
C₁₆H₁₃N₅O

Purity:
≥98% (HPLC)

Appearance:
Light yellow powder

Solubility:
DMSO (100mg/ml)

Method for Determining Identity:
Proton NMR Spectroscopic and LC-MS Spectrometric Analysis

Carbon:
62-67%

Hydrogen:
4-6%

Nitrogen:
22-25%

Water by CHN (mol):
≥0.0mol

Primary Target:
CFTR

Storage and Stability:
May be stored at 4°C. For long-term storage, aliquot and store at 4°C. Do not freeze.