Uses
A922500 has been used in the inhibition of diacylglycerol acyltransferase (DGAT) in epithelial human breast cancer cell line (MDA-MB-231), digitonin-permeabilized human cancer cells, human myotubes and macrophages.
Definition
ChEBI: A 922500 is an aromatic ketone.
Biological Activity
Diacylglycerol acyltransferase 1 (DGAT-1) inhibitor (IC 50 values are 7 and 24 nM at human and mouse DGAT-1 respectively) that is devoid of activity at DGAT-2, ACAT1 or ACAT2. Induces significant weight loss without altering food intake, and decreases liver and plasma triglyceride levels in vivo . Orally active.
Biochem/physiol Actions
The diacylglycerol acyltransferase (DGAT) 1 inhibitor A922500 was shown to effectively reduce postprandial serum triglyceride levels in rodents at concentrations of 0.03, 0.3 and 3 mg/kg. These results suggest A922500 may have beneficial effects in reducing the risk of cardiovascular disease.
