NG-497 is a potent, highly selective, nontoxic inhibitor of human adipose triglyceride lipase (ATGL, PNPLA2) with IC50 of 1 uM.
NG-497 dose-dependently inhibits TAG hydrolase activity of human ATGL.
NG-497 does not inhibit other TAG hydrolases of the PNPLA family and human acylglycerol hydrolases.
NG-497 also inhibits rhesus monkey ATGL, but has no substantial effects on ATGL orthologues from mouse, rat, goat, pig, dog, and marmoset.
NG-497 dose-dependent decreases isoproterenol-stimulated atty acids (FAs) and glycerol release in human SGBS (IC50=1.5 uM) and primary human adipocytes.
NG-497 reduces lipolysis-dependent respiration of HepG2 cells and does not compromise mitochondrial function via off-target effects.
