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Description: Atglistatin is a highly potent and selective inhibitor of adipose triglyceride lipase (ATGL) with IC50 of 0.7 uM, it showed high selectivity over other key metabolic lipases. In lysates from E. coli overexpressing ATGL, atglistatin inhibited ATGL activity with IC50 value of 0.7 uM. Atglistatin at concentrations up to 50 uM had no cytotoxicity. Also, atglistatin inhibited ATGL with Ki value of 355 nM in a competitive way. In white adipose tissue (WAT) lysates of wild-type mice, atglistatin inhibited triacylglycerol (TG) hydrolase activity by 78%. The combination of Atglistatin and the HSL inhibitor Hi 76-007917 inhibited TG hydrolase activity by 95%.
References: Nat Chem Biol. 2013 Dec; 9(12):785-7.
Chemical Name: 3-(4'-(dimethylamino)-[1, 1'-biphenyl]-3-yl)-1, 1-dimethylurea
InChi Key: AWOPBSAJHCUSAS-UHFFFAOYSA-N
InChi Code: InChI=1S/C17H21N3O/c1-19(2)16-10-8-13(9-11-16)14-6-5-7-15(12-14)18-17(21)20(3)4/h5-12H, 1-4H3, (H, 18, 21)
SMILES Code: CN(C1=CC=C(C=C1)C2=CC(NC(N(C)C)=O)=CC=C2)C
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