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534335 ACC1/2 Inhibitor, Cpd 9

534335
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Aperçu

Replacement Information

Tableau de caractéristiques principal

Empirical Formula
C₂₃H₂₇N₅O₂

Products

RéférenceConditionnement Qté
5343350001 Flacon en verre 10 mg
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
Global Trade Item Number
Référence GTIN
5343350001 04054839116414

Documentation

ACC1/2 Inhibitor, Cpd 9 FDS

Titre

Fiche de données de sécurité des matériaux (FDS) 

Références bibliographiques

Aperçu de la référence bibliographique
Griffith, D.A., et al. 2014. J. Med. Chem. 57, 10512.
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.

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 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 3 months at -20°C.
Toxicity Standard Handling
ReferencesGriffith, D.A., et al. 2014. J. Med. Chem. 57, 10512.