Atglistatin is a highly effective, specific and competitive ATGL inhibitor with an IC50 of ~0.7 μM for inhibition of lipolysis in vitro, and no toxicity when the concentration up to 50 μM.

ATGL:0.7 μM

Atglistatin可抑制ATGL,从而使细胞和器官培养中的脂类分解受到抑制,且浓度达50 μM时仍无细胞毒性。

Atglistatin（p.o.）剂量依赖性地减少FA和甘油,减少量分别高达50%和62%,也会显著减少血浆中TG水平（43%）.在体内,Atglistatin(i.p.)剂量与时间依赖性地抑制脂类分解.此外,Atglistatin有明显的组织分布差异,主要在肝脏和脂肪组织中积累。

Determination of lipase activity: For determination of lipase activity, lysates are incubated with a substrate containing radiolabeled [9,10-3H(N)]-triolein. Subsequently, FA are extracted and quantitated by liquid scintilation counting. Data are presented as mean S.D. of triplicate determinations and representative for at least three independent experiments.

For MTT-based in vitro viability assays, cells are seeded in 96-well plates and cultured under standard conditions for 24 h. The next day, cells are pretreated with different concentrations of Atglistatin dissolved in DMSO or Cisplatin dissolved in DMF as positive control for 2 h. Medium is replaced by an identical fresh medium and incubated again for the indicated time points. Thereafter, cells are incubated for 3 h with 100 μL Thiazolyl Blue Tetrazolium Bromide (MTT). The resulting violet formazan crystals are dissolved by adding 100 μL of MTT solubilization solution (0.1% NP-40, 4 mM HCl and anhydrous isopropanol). After complete dissolution of the formazan product, absorbance is measured at 595 nm using 690 nm as reference wavelength.(Only for Reference)