Administered orally in olive oil, Atglistatin influences plasma and tissue TG levels, among other metabolic parameters, in animals. Lipolytic indicators such as fatty acids (FA) and glycerol show reductions 4 and 8 hours post-administration, with levels returning to baseline after 12 hours. A dose-dependent decrease in FA and glycerol, up to 50% and 62% respectively, is observed 8 hours following treatment. Additionally, Atglistatin significantly lowers plasma TG levels by 43% without affecting blood glucose, total cholesterol, ketone bodies, and insulin levels. These effects are also seen when Atglistatin is administered via intraperitoneal injection, highlighting its potential as an anti-lipolytic agent^[1].

Atglistatin targets the triacylglycerol (TG) hydrolase activity of adipose triglyceride lipase (ATGL) in white adipose tissue (WAT), inhibiting it in a dose-dependent manner and achieving up to a 78% reduction at the highest tested concentration. In WAT lysates from ATGL knockout (ko) animals, where TG hydrolase activity is already diminished by about 70%, Atglistatin exerts a moderate effect on the remaining activity. This suggests that the majority of the non-ATGL related TG hydrolase activity can be attributed to hormone-sensitive lipase (HSL), especially since the combined inhibition with Atglistatin and an HSL inhibitor nearly abolishes TG hydrolase activity in WAT (-95%)^[1].