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481908 Nicotinamide Phosphoribosyltransferase Inhibitor, FK866 - CAS 658084-64-1 - Calbiochem

The Nicotinamide Phosphoribosyltransferase Inhibitor, FK866, also referenced under CAS 658084-64-1, controls the biological activity of Nicotinamide Phosphoribosyltransferase. This small molecule/inhibitor is primarily used for Neuroscience applications.

FDS (Fiches de données de sécurité), certificats d’analyse (CoA) et de qualité (CoQ), dossiers, brochures et autres documents disponibles.

Synonymes: NAPRT Inhibitor, (E)-N-(4-(1-Benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide, NAMPT Inhibitor, APO866, NAMPTase Inhibitor I, PBEF Inhibitor I, Visfatin Inhibitor I

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481908
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Tableau de caractéristiques principal

CAS #Empirical Formula
658084-64-1C₂₄H₂₉N₃O₂

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      Description
      OverviewA cell-permeable pyridinylacrylamide compound that acts as a selective, allosteric NAPRT/NAMPT (nicotinamide phosphoribosyltransferase) inhibitor (Ki = 0.4 nM for the enzyme/substrate complex; Ki′ = 0.3 nM for the free enzyme), while exhibiting no effect toward NPRT (nicotinic acid phosphoribosyltransferase) activity (82% inhibition of NAPRT activity at 10 nM vs no inhibition of NPRT activity at 1 µM in K-562 extract). FK866 treatment is shown to induce cell death by depleting NAD+ (Cat. Nos. 481911 & 481915) in HepG2 and NIH-3T3 cultures (by >95% after 24 h treatment of 10 nM FK866), likewise the addition of exogenous NAD+ is demonstrated to rescue NIH-3T3 and SH-SY5Y from FK866-induced NAD+-depletion and cell death.
      Catalogue Number481908
      Brand Family Calbiochem®
      SynonymsNAPRT Inhibitor, (E)-N-(4-(1-Benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide, NAMPT Inhibitor, APO866, NAMPTase Inhibitor I, PBEF Inhibitor I, Visfatin Inhibitor I
      References
      ReferencesFormentini, L., et al. 2009. Biochem. Pharmacol. 77, 1612.
      Nakahata, Y., et al. 2009. Science 324, 654.
      Ramsey. K.M., et al. 2009. Science 324, 651.
      Billington, R.A., et al. 2008. J. Biol. Chem. 283, 6367.
      Hasmann, M. and Schemainda, I., 2003. Cancer Res. 63, 7436.
      Product Information
      CAS number658084-64-1
      FormColorless to yellow liquid
      FormulationSupplied as a 50 mM (2 mg/102.17 µl) solution in DMSO.
      Hill FormulaC₂₄H₂₉N₃O₂
      Chemical formulaC₂₄H₂₉N₃O₂
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Purity≥97% by HPLC
      Physicochemical Information
      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
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications
      Global Trade Item Number
      Référence GTIN
      481908-2MG 04055977225532

      Documentation

      Nicotinamide Phosphoribosyltransferase Inhibitor, FK866 - CAS 658084-64-1 - Calbiochem FDS

      Titre

      Fiche de données de sécurité des matériaux (FDS) 

      Nicotinamide Phosphoribosyltransferase Inhibitor, FK866 - CAS 658084-64-1 - Calbiochem Certificats d'analyse

      TitreNuméro de lot
      481908

      Références bibliographiques

      Aperçu de la référence bibliographique
      Formentini, L., et al. 2009. Biochem. Pharmacol. 77, 1612.
      Nakahata, Y., et al. 2009. Science 324, 654.
      Ramsey. K.M., et al. 2009. Science 324, 651.
      Billington, R.A., et al. 2008. J. Biol. Chem. 283, 6367.
      Hasmann, M. and Schemainda, I., 2003. Cancer Res. 63, 7436.
      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.

      Revision06-May-2020 JSW
      SynonymsNAPRT Inhibitor, (E)-N-(4-(1-Benzoylpiperidin-4-yl)butyl)-3-(pyridin-3-yl)acrylamide, NAMPT Inhibitor, APO866, NAMPTase Inhibitor I, PBEF Inhibitor I, Visfatin Inhibitor I
      DescriptionA cell-permeable pyridinylacrylamide compound that acts as a selective, allosteric NAPRT/NAMPT (nicotinamide phosphoribosyltransferase) inhibitor (Ki = 0.4 nM for the enzyme/substrate complex; Ki′ = 0.3 nM for the free enzyme), while exhibiting no effect toward NPRT (nicotinic acid phosphoribosyltransferase) activity (82% inhibition of NAPRT activity at 10 nM vs no inhibition of NPRT activity at 1 µM in K-562 extract). FK866 treatment is shown to induce cell death by depleting NAD+ (Cat. Nos. 481911 & 481915) in HepG2 and NIH-3T3 cultures (by >95% after 24 h treatment of 10 nM FK866), likewise the addition of exogenous NAD+ is demonstrated to rescue NIH-3T3 and SH-SY5Y from FK866-induced NAD+-depletion and cell death.
      FormColorless to yellow liquid
      FormulationSupplied as a 50 mM (2 mg/102.17 µl) solution in DMSO.
      Intert gas (Yes/No) Packaged under inert gas
      CAS number658084-64-1
      Chemical formulaC₂₄H₂₉N₃O₂
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (100 mg/ml)
      Storage Protect from light
      +2°C to +8°C
      Do Not Freeze Ok to freeze
      Toxicity Standard Handling
      ReferencesFormentini, L., et al. 2009. Biochem. Pharmacol. 77, 1612.
      Nakahata, Y., et al. 2009. Science 324, 654.
      Ramsey. K.M., et al. 2009. Science 324, 651.
      Billington, R.A., et al. 2008. J. Biol. Chem. 283, 6367.
      Hasmann, M. and Schemainda, I., 2003. Cancer Res. 63, 7436.