534335 ACC1/2 Inhibitor, Cpd 9

534335
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical Formula
      C₂₃H₂₇N₅O₂

      Pricing & Availability

      Catalog Number AvailabilityPackaging Qty/Pack Price Quantity
      5.34335.0001
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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
          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.