A922500 959122-11-3

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Molecular Weight:

428.48 A922500 is an inhibitor for human and mouse DGAT-1 with IC50 of 7 nM and 24 nM, respectively, good selectivity over related acyltransferases, hERG, and a panel of anti-targets.






Biological Activity


A 922500 inhibits the phylogenetic family members acyl coenzyme A cholesterol acyltransferase-1 and -2 with IC50 of 296 μM. [1] A 922500 potently inhibits huDGAT-1 and mseDGAT-1.


Zucker fatty rats and diet-induced dyslipidemic hamsters are dosed
orally with A 922500 (0.03, 0.3, and 3 mg/kg) for 14 days. Serum
triglycerides ae significantly reduced by the 3 mg/kg dose of A 922500
in both the Zucker fatty rat (39%) and hyperlipidemic hamster (53%).
These serum triglyceride changes are accompanied by significant
reductions in free fatty acid levels by 32% in the Zucker fatty rat and
55% in the hyperlipidemic hamster.


In addition, high-density
lipoprotein-cholesterol is significantly increases (25%) in the Zucker
fatty rat by A 922500 administered at 3 mg/kg. A 922500
confers weight loss and a reduction in liver triglycerides when dosed
chronically in DIO mice and depletes serum triglycerides following a
lipid challenge in a dose-dependent manner, thus, reproducing major
phenotypical characteristics of DGAT-1(-/-) mice. A
922500 (0.03, 0.3 and 3 mg/kg, p.o.) dose-dependently attenuates the
maximal postprandial rise in serum triglyceride concentrations.

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Product Categories : Metabolism > Transferase Inhibitor