505479 | SIRT1/2/3 pan Inhibitor - Calbiochem

SIRT1/2/3 pan Inhibitor - Calbiochem MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

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

Primary Target: SIRT1/2/3
505479
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      Overview

      Replacement Information

      Key Spec Table

      Empirical Formula
      C₁₉H₂₇N₅O₂S

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      Catalogue NumberAvailability Packaging Qty/Pack Price Quantity
      5.05479.0001
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          		Glass bottle 10 mg
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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
          FormPale yellow powder
          Hill FormulaC₁₉H₂₇N₅O₂S
          Chemical formulaC₁₉H₂₇N₅O₂S
          ReversibleY
          Structure formula Image
          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

          Documentation

          SDS

          Title

          Safety Data Sheet (SDS) 

          References

          Reference overview
          Disch, J.S., et al. 2013. J. Med. Chem. 57, 1275.
          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.

          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
          Chemical formulaC₁₉H₂₇N₅O₂S
          Structure formula
          Purity≥97% by HPLC
          SolubilityDMSO (10 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
          ReferencesDisch, J.S., et al. 2013. J. Med. Chem. 57, 1275.