a-922500

A-922500 is a potent, selective, and orally bioavailable small-molecule inhibitor of diacylglycerol acyltransferase 1 (DGAT-1), the enzyme responsible for catalyzing the final step in triglyceride synthesis[1]. It has demonstrated high potency and selectivity, with IC50 values of 7 nM and 24 nM for human and mouse DGAT-1, respectively, and minimal activity against related acyltransferases or off-targets[1][3][5]. In preclinical rodent models, A-922500 significantly reduces serum triglyceride and free fatty acid levels, increases HDL-cholesterol, induces weight loss, and depletes liver triglycerides, recapitulating the phenotype of DGAT-1 knockout animals[1][3]. Originally developed by Abbott Laboratories for metabolic diseases, A-922500 has been used in research on obesity, dyslipidemia, and postprandial hyperlipidemia, but its clinical development status is not advanced—currently listed as "Pending" with no marketed products or approved indications[9]. The compound is also used in cancer research, where it has been shown to increase oxidative stress and activate the NRF2/SESN2 pathway in certain tumor models, though without significant impact on tumor growth in vivo[2].

Other names

DGAT-1 Inhibitor 4aDGAT1 Inhibitor 4aDGAT 1 Inhibitor 4a