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530541 CFTR Potentiator, VX-770 - CAS 873054-44-5 - Calbiochem

A cell-permeable, potentiator of CFTR that directly, reversibly, and allosterically binds to WT and G551D mutant forms (~ 10 µM) and increases the open probability to restore lung function.

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Synonymes: Cystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco, N-(5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide

Primary Target: WT and G551D mutant forms of cell surface CFTR
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530541
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Tableau de caractéristiques principal

CAS #Empirical Formula
873054-44-5C₂₄H₂₈N₂O₃

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      Description
      OverviewA cell-permeable, orally bioavailable dihydroquinoline-carboxamide compound that acts as a potentiator of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by directly binding to WT and G551D mutant forms in an allosteric and reversible manner (~ 10 µM) and increases the open probability to restore lung function. Enhances cAMP/PKA-signaling mediated gating activity of both WT and G551D mutants and its potentiation activity is dependent upon the phosphorylated status of CFTR. Does not compete for binding to the canonical ATP-binding catalytic site; but the rate of flux through CFTR increase by 1.5 to 2 fold when ATP concentrations are increased. Shown to increase Cl- secretion by about 10 fold in cultured human CF bronchial epethelia (HBE) carrying G551D/F508del mutations and increases forskolin-stimulated transepethial current (IT; EC50 = 236 nM) far more effectively than genistein (EC50 = 16 µM). Displays favorable pharmacokinetic properties with t1/2= 12 h.

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number530541
      Brand Family Calbiochem®
      SynonymsCystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco, N-(5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide
      References
      ReferencesNamkung, W., et al. 2013. Mol. Pharmacol. 84, 384.
      Eckford, P.D.W., et al. 2012. J. Biol. Chem. 287, 36639.
      Van Goor, F., et al 2009. Proc. Natl. Acad. Sci. USA 106, 18825.
      Product Information
      CAS number873054-44-5
      FormOff-white powder
      Hill FormulaC₂₄H₂₈N₂O₃
      Chemical formulaC₂₄H₂₈N₂O₃
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetWT and G551D mutant forms of cell surface CFTR
      Purity≥98% by HPLC
      Physicochemical Information
      Cell permeableY
      Dimensions
      Materials Information
      Toxicological Information
      Safety Information according to GHS
      Safety Information
      Product Usage Statements
      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
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      5305410001 04055977260908

      Documentation

      CFTR Potentiator, VX-770 - CAS 873054-44-5 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Références bibliographiques

      Aperçu de la référence bibliographique
      Namkung, W., et al. 2013. Mol. Pharmacol. 84, 384.
      Eckford, P.D.W., et al. 2012. J. Biol. Chem. 287, 36639.
      Van Goor, F., et al 2009. Proc. Natl. Acad. Sci. USA 106, 18825.
      Fiche technique

      Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

      Revision13-June-2014 JSW
      SynonymsCystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco, N-(5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide
      DescriptionA cell-permeable, orally bioavailable dihydroquinoline-carboxamide compound that acts as a potentiator of Cystic Fibrosis Transmembrane Conductance Regulator (CFTR) by directly binding to WT and G551D mutant forms in an allosteric and reversible manner (~ 10 µM) and increases the open probability to restore lung function. Enhances cAMP/PKA-signaling mediated gating activity of both WT and G551D mutants and its potentiation activity is dependent upon the phosphorylated status of CFTR. Does not compete for binding to the canonical ATP-binding catalytic site; but the rate of flux through CFTR increase by 1.5 to 2 fold when ATP concentrations are increased. Shown to increase Cl- secretion by about 10 fold in cultured human CF bronchial epethelia (HBE) carrying G551D/F508del mutations and increases forskolin-stimulated transepethial current (IT; EC50 = 236 nM) far more effectively than genistein (EC50 = 16 µM). Displays favorable pharmacokinetic properties with t1/2= 12 h.
      FormOff-white powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number873054-44-5
      Chemical formulaC₂₄H₂₈N₂O₃
      Structure formulaStructure formula
      Purity≥98% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      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.
      Toxicity Standard Handling
      ReferencesNamkung, W., et al. 2013. Mol. Pharmacol. 84, 384.
      Eckford, P.D.W., et al. 2012. J. Biol. Chem. 287, 36639.
      Van Goor, F., et al 2009. Proc. Natl. Acad. Sci. USA 106, 18825.