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505479 SIRT1/2/3 pan Inhibitor - CAS 1431411-60-7 - Calbiochem

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Synonyme: pan SIRT1/2/3 Inhibitor, 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide

Primary Target: SIRT1/2/3
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505479
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Übersicht

Replacement Information

Key Spec Table

CAS #Empirical Formula
1431411-60-7C₁₉H₂₇N₅O₂S

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      Description
      OverviewA thienopyrimidinylcarboxamide that acts as a highly potent, reversible pan sirtuin (SIRT) inhibitor (IC50 = 15, 10, and 33 nM for SIRT1, 2, and 3, respectively). Shown to bind to the SIRT catalytic site and occupy both the nicotinamide C-pocket and acetyl lysine substrate channel. Exhibits high selectivity over a panel of protein kinases, nuclelar receptors, GPCRs, and ion-channels (IC50 > 10 µM). Poorly affects hERG and cytochrome P450s (> 50 µM). Exhibits desirable stability in microsomal preparations (human CLint = 15.8 µL/min/mg, mouse CLint = 12.7 µL/min/mg) and high solubility (297 µM), and low LogD (2.73).
      Catalogue Number505479
      Brand Family Calbiochem®
      Synonymspan SIRT1/2/3 Inhibitor, 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide
      References
      ReferencesDisch, J.S., et al. 2013. J. Med. Chem. 57, 1275.
      Product Information
      CAS number1431411-60-7
      FormPale yellow powder
      Hill FormulaC₁₉H₂₇N₅O₂S
      Chemical formulaC₁₉H₂₇N₅O₂S
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetSIRT1/2/3
      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
      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
      Bestellnummer GTIN
      5.05479.0001 04055977243871

      Documentation

      SIRT1/2/3 pan Inhibitor - CAS 1431411-60-7 - Calbiochem SDB

      Titel

      Sicherheitsdatenblatt (SDB) 

      Literatur

      Übersicht
      Disch, J.S., et al. 2013. J. Med. Chem. 57, 1275.
      Datenblatt

      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.

      Revision22-November-2013 JSW
      Synonymspan SIRT1/2/3 Inhibitor, 4-(4-(2-Pivalamidoethyl)piperidin-1-yl)thieno[3,2-d]pyrimidine-6-carboxamide
      DescriptionA thienopyrimidinylcarboxamide that acts as a highly potent, reversible pan sirtuin (SIRT) inhibitor (IC50 = 15, 10, and 33 nM for SIRT1, 2, and 3, respectively). Shown to bind to the SIRT catalytic site and occupy both the nicotinamide C-pocket and acetyl lysine substrate channel. Exhibits high selectivity over a panel of protein kinases, nuclelar receptors, GPCRs, and ion-channels (IC50 > 10 µM). Poorly affects hERG and cytochrome P450s (> 50 µM). Exhibits desirable stability in microsomal preparations (human CLint = 15.8 µL/min/mg, mouse CLint = 12.7 µL/min/mg) and high solubility (297 µM), and low LogD (2.73).
      FormPale yellow powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1431411-60-7
      Chemical formulaC₁₉H₂₇N₅O₂S
      Structure formulaStructure formula
      Purity≥97% by HPLC
      SolubilityDMSO (10 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
      ReferencesDisch, J.S., et al. 2013. J. Med. Chem. 57, 1275.