5.34335
ACC1/2 Inhibitor, Cpd 9
Synonym(s):
ACC1/2 Inhibitor, Cpd 9, ACC Inhibitor, Cpd9, Acetyl-CoA Carboxylase Inhibitor, Cpd9
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About This Item
Empirical Formula (Hill Notation):
C23H27N5O2
Molecular Weight:
405.49
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥98% (HPLC)
Form:
solid
Storage condition:
OK to freeze, protect from light
assay
≥98% (HPLC)
Quality Segment
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
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 (t1/2 = 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
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)
Storage Class
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Certificates of Analysis (COA)
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