NG-497 is a non-cytotoxic, substrate-competitive, reversible and highly selective human/primate adipose triglyceride lipase (ATGL; IPLA2-zeta; PNPLA2) inhibitor (IC50 = 1 μM, Ki = 0.5 μM) with little activity toward related human lipid hydrolases or ATGL orthologues from other species (<20% inhibition of mouse, rat, goat, pig, dog, marmoset ATGL at 50 μM). NG-497 abolishes hormone-induced lipolysis in human adipocytes (IC50 = 1.5 and 0.5 μM against 1 μM isoproterenol-induced total or hormonesensitive lipase (HSL)-independent FA release in Simpson-Golabi-Behmel syndrome adipocytes), but not in HepG2 that lacks ATGL hydrolase activity.
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Journal of the American Chemical Society, 144(14), 6237-6250 (2022-04-02)
Chronically elevated circulating fatty acid levels promote lipid accumulation in nonadipose tissues and cause lipotoxicity. Adipose triglyceride lipase (ATGL) critically determines the release of fatty acids from white adipose tissue, and accumulating evidence suggests that inactivation of ATGL has beneficial
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