Atglistatin

Research use only, not for human use.

Atglistatin is a highly potent, selective and competitive inhibitor of adipose triglyceride lipase (ATGL) with an IC50 of ~0.7 μM for inhibition of lipolysis in vitro, but no toxicity up to a concentration of 50 μM.

Atglistatin is a highly potent, selective and competitive inhibitor of adipose triglyceride lipase (ATGL) with an IC50 of ~0.7 μM for inhibition of lipolysis in vitro, but no toxicity up to a concentration of 50 μM.(In Vitro):Atglistatin inhibits Triacylglycerol (TG) hydrolase activity of wild-type white adipose tissue (WAT) in a dose-dependent manner up to 78% at the highest concentration. In comparison to wild-type preparations, TG hydrolase activity in WAT lysates from ATGL-ko animals is reduced by approximately 70% and Atglistatin had only a moderate effect on the residual activity. The combined use of Atglistatin and the hormone-sensitive lipase (HSL) inhibitor Hi 76-0079 leads to an almost complete inhibition (-95%) of TG hydrolase activity of WAT which implicates that most of the non-ATGL activity can be ascribed to HSL.(In Vivo):Animals receive Atglistatin dissolved in olive oil by oral gavage. After application, blood and tissues are collected for determination of plasma parameters, tissue Triacylglycerol (TG) levels, and inhibitor concentrations. Time-course experiments revealed that the lipolytic parameters fatty acids (FA) and glycerol are reduced 4 and 8 hours after application and returned to normal after 12 hours. Eight hours after treatment, a dose-dependent decrease is observed in FA and glycerol levels up to 50% and 62%, respectively. Atglistatin also caused a strong reduction in plasma TG levels (-43%) while blood glucose, total cholesterol, ketone bodies, and insulin levels do not significantly change. Dose and time-dependent inhibition of lipolysis is also observed in response to intraperitoneal injection of Atglistatin.

——

——

Atglistatin

Metabolic Enzyme/Protease

Lipase

ATGL

Metabolic Disease

——

1469924-27-3

283.37

C17H21N3O

>98% (HPLC)

Ethanol: 4 mg/mL (14.11 mM); DMSO: 57 mg/mL (201.15 mM)

CN(C1=CC=C(C=C1)C2=CC(NC(N(C)C)=O)=CC=C2)C

3-(4'-(dimethylamino)-[1,1'-biphenyl]-3-yl)-1,1-dimethylurea

(-20℃)

With Ice Pack

≥ 2 years