Add time:07/24/2019         Source:sciencedirect.com

Adipose triglyceride lipase (ATGL) catalyzes the degradation of cellular triacylglycerol stores and strongly determines the concentration of circulating fatty acids (FAs). High serum FA levels are causally linked to the development of insulin resistance and impaired glucose tolerance, which eventually progresses to overt type 2 diabetes. ATGL-specific inhibitors could be used to lower circulating FAs, which can counteract the development of insulin resistance. In this article, we report about structure–activity relationship (SAR) studies of small molecule inhibitors of ATGL based on a hydrazone chemotype. The SAR indicated that the binding pocket of ATGL requests rather linear compounds without bulky substituents. The best inhibitor showed an IC50 = 10 μM in an assay with COS7-cell lysate overexpressing murine ATGL.

We also recommend Trading Suppliers and Manufacturers of 4-Aminobenzaldehyde phenyl hydrazone (cas 19098-48-7). Pls Click Website Link as below: cas 19098-48-7 suppliers