5.34335

ACC1/2 Inhibitor, Cpd 9

• Synonym(e): ACC1/2 Inhibitor, Cpd 9, ACC Inhibitor, Cpd9, Acetyl-CoA Carboxylase Inhibitor, Cpd9
• Empirische Formel (Hill-System): C₂₃H₂₇N₅O₂
• Molekulargewicht: 405.49
• NACRES: NA.77
• UNSPSC Code: 12352200
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: OK to freeze, protect from light

Eigenschaften

• assay: ≥98% (HPLC)
• Quality Segment: 100
• form: solid
• manufacturer/tradename: Calbiochem^®
• storage condition: OK to freeze, protect from light
• color: tan
• solubility: DMSO: 100 mg/mL
• storage temp.: 2-8°C

Beschreibung

General description

A 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 (t_1/2 = 4.8 h in rat and 5.7 h in dog, at 3 mg/kg, p.o.).

Biochem/physiol Actions

Cell permeable: yes

Primary Target
ACC

Preparation Note

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

Other Notes

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

Legal Information

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

Disclaimer

Toxicity: Standard Handling (A)

Sicherheitshinweise

• Lagerklasse: 11 - Combustible Solids
• wgk: WGK 3
• flash_point_f: Not applicable
• flash_point_c: Not applicable