NG-497 is the first small molecule inhibitor (IC50 = 1 µM) of human and rhesus monkey adipose triglyceride lipase (ATGL). It is inactive against mouse, rat, goat, pig, dog, and marmoset ATGL orthologues. Of the eight enzymes expressed by humans in the patatin-like phospholipase domain-containing (PNPLA) protein family, NG-497 was selective for PNPLA 2 (ATGL). NG-497 was also inactive against HSL, CES2, LPL, and HL. Reversible and non-toxic.
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