product name Atglistatin
Description: Atglistatin is a highly potent, and selective inhibitor of adipose triglyceride lipase (ATGL) with IC50 of 0.7 μM, 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 μM. Atglistatin at concentrations up to 50 μM 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.
283.37
Formula
C17H21N3O
CAS No.
1469924-27-3
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 57 mg/mL (201.2 mM)
Water: <1 mg/mL
Ethanol: 4 mg/mL (14.1 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: Atglistatin inhibits lipolysis in cell and organ cultures by targeting ATGL with no cytotoxicity up to a concentration of 50 μM. Kinase Assay: 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. Cell Assay: 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. |
|---|---|
| In Vivo | In vivo, Atglistatin (i.p.) results in Dose and time-dependent inhibition of lipolysis. Oral treatment of Atglistatin causes a dose-dependent decrease in FA and glycerol of up to 50% and 62%, respectively, and also causes a strong reduction in plasma TG levels (43%). In addition, Atglistatin shows a distinct tissue distribution and primarily accumulates in liver and adipose tissue. |
| Animal model | Mice (C57Bl/6J) |
| Formulation & Dosage | Formulated in Olive oil (oral gavage), PBS containing 0.25% Cremophor EL (i.p.); 1.4 mg/mouse (oral gavage); ~400 μmol/kg (i.p.); oral gavage or i.p. |
| References | Nat Chem Biol. 2013 Dec;9(12):785-7. |
