5.34335

ACC1/2 Inhibitor, Cpd 9

• Synonyme(s) : ACC1/2 Inhibitor, Cpd 9, ACC Inhibitor, Cpd9, Acetyl-CoA Carboxylase Inhibitor, Cpd9
• Formule empirique (notation de Hill): C₂₃H₂₇N₅O₂
• Poids moléculaire : 405.49
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Pureté: ≥98% (HPLC)
• Niveau de qualité: 100
• Forme: solid
• Fabricant/nom de marque: Calbiochem^®
• Conditions de stockage: OK to freeze; protect from light
• Couleur: tan
• Solubilité: DMSO: 100 mg/mL
• Température de stockage: 2-8°C

Description

Description générale

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.).

Actions biochimiques/physiologiques

Cell permeable: yes

Primary Target
ACC

Avertissement

Toxicity: Standard Handling (A)

Reconstitution

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

Autres remarques

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

Informations légales

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

Informations sur la sécurité

• Code de la classe de stockage: 11 - Combustible Solids
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable