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

530541
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₄H₂₈N₂O₃ 873054-44-5

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      5.30541.0001
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          Glass bottle 10 mg
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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®
          SynonymsN-(5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide, Cystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco
          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
          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

          Documentation

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

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          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.
          Data Sheet

          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
          SynonymsN-(5-Hydroxy-2,4-bis(2-methyl-2-propanyl)phenyl]-4-oxo-1,4-dihydro-3-quinolinecarboxamide, Cystic Fibrosis Transmembrane Conductance Regulator Potentiator, VX 770, Ivacaftor, Kalydeco
          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 +2°C to +8°C
          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.
          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.