ABT-046 is an orally active, selective, and highly efficient Diacylglycerol Acyltransferase 1 (DGAT-1) inhibitor that can be used in metabolic disease research.

DGAT-1 (human):78 nM

ABT-046 did not significantly inhibit human DGAT-2, but prevented human DGAT-1 from catalyzing triglyceride production in HeLa cells, with an IC50 of 78 nM.[1]
In Caco-2 cells, ABT-046 exhibited high in vitro permeability and no active efflux was detected (efflux ratios of 1.4 and 1.1 at 0.5 and 5 μM, respectively).[1] ABT-046 was also found to inhibit human DGAT-2, but prevented human DGAT-1 from catalyzing triglyceride production in HeLa cells with an IC50 of 78 nM. [1]
The metabolic conversion of ABT-046 to mouse and human liver microsomes is extremely low and almost negligible. [1]

Single gavage administration of ABT-046 (0.03-3 mg/kg) significantly reduced postprandial triglyceride levels in CD-1 mice. [1]
Single gavage administration of ABT-046 (0.3 mg/kg) effectively suppressed postprandial triglyceride fluctuations in diet-induced obese mice. [1]