534335 ACC1/2 Inhibitor, Cpd 9

534335
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Overview

Replacement Information

Key Spec Table

Empirical Formula
C₂₃H₂₇N₅O₂

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      Glass bottle 10 mg
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      Description
      OverviewA cell-permeable, spiral ketone derivative that acts as a highly potent inhibitor of acetyl-CoA carboxylase (ACC; IC50 = 27 and 33 nM for human ACC1 and ACC2, respectively). The inhibition appears to be uncompetitive with respect to ATP and non-competitive with carbonate and acetyl-CoA. Inhibits malonyl-CoA synthesis in primary rat hepatocytes (IC50 = 29.9 nM) and reduces de novo hepatic lipid synthesis (ED50 = 7.8 mg/kg in rats). Acutely reduces whole body respiratory exchange ratio (RER) to indicate a switch to fatty acid utilization. Has low protein binding in rat and dog plasma, but exhibits about 10-fold higher binding in monkey and human plasma. Displays favorable pharmacokinetic properties with good bioavailability, microsomal stability, and low plasma clearance (t1/2 = 4.8 h in rat and 5.7 h in dog, at 3 mg/kg, p.o.).
      Catalogue Number534335
      Brand Family Calbiochem®
      SynonymsACC Inhibitor, Cpd9, Acetyl-CoA Carboxylase Inhibitor, Cpd9
      References
      ReferencesGriffith, D.A., et al. 2014. J. Med. Chem. 57, 10512.
      Product Information
      FormTan solid
      Hill FormulaC₂₃H₂₇N₅O₂
      Chemical formulaC₂₃H₂₇N₅O₂
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetACC
      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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      ACC1/2 Inhibitor, Cpd 9 SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Griffith, D.A., et al. 2014. J. Med. Chem. 57, 10512.
      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.

      Revision26-June-2017 JSW
      SynonymsACC Inhibitor, Cpd9, Acetyl-CoA Carboxylase Inhibitor, Cpd9
      DescriptionA cell-permeable, spiral ketone derivative that acts as a highly potent inhibitor of acetyl-CoA carboxylase (ACC; IC50 = 27 and 33 nM for human ACC1 and ACC2, respectively). The inhibition appears to be uncompetitive with respect to ATP and non-competitive with carbonate and acetyl-CoA. Inhibits malonyl-CoA synthesis in primary rat hepatocytes (IC50 = 29.9 nM) and reduces de novo hepatic lipid synthesis (ED50 = 7.8 mg/kg in rats). Acutely reduces whole body respiratory exchange ratio (RER) to indicate a switch to fatty acid utilization. Has low protein binding in rat and dog plasma, but exhibits about 10-fold higher binding in monkey and human plasma. Displays favorable pharmacokinetic properties with good bioavailability, microsomal stability, and low plasma clearance (t1/2 = 4.8 h in rat and 5.7 h in dog, at 3 mg/kg, p.o.).
      FormTan solid
      Intert gas (Yes/No) Packaged under inert gas
      Chemical formulaC₂₃H₂₇N₅O₂
      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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesGriffith, D.A., et al. 2014. J. Med. Chem. 57, 10512.