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505985 CFTR Activator, Cact-A1 - CAS 354576-90-2 - Calbiochem

Overview

Key Spec Table

CAS #Empirical Formula
354576-90-2C₁₆H₁₃N₅O

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      Glass bottle 10 mg
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      Description
      OverviewA 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 = 1.6 µM in CFTR-expressing Fisher rat thyroid cells). Also shown to activate ΔF508-CFTR in primary CF-HBE cell cultures (EC50 = 3.5 µM). Reported to directly bind to the same site as CFTRinh-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.
      Catalogue Number505985
      Brand Family Calbiochem®
      Synonyms5-((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, Cystic Fibrosis Transmembrane Conductance Regulator Activator, Cact-A1
      References
      ReferencesNamkung, W., et al. 2013. Mol. Pharmacol. 84, 384.
      Product Information
      CAS number354576-90-2
      FormLight yellow powder
      Hill FormulaC₁₆H₁₃N₅O
      Chemical formulaC₁₆H₁₃N₅O
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetCFTR
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Catalogue Number GTIN
      5.05985.0001 04055977262575