Atglistatin

Catalog No.S7364

Atglistatin Chemical Structure

Molecular Weight(MW): 283.37

Atglistatin is a highly potent, and selective inhibitor of adipose triglyceride lipase (ATGL) with IC50 of 0.7 μM, high selectivity over other key metabolic lipases.

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  • C, G0s2-null MEFs were transfected with HRAS and the following day treated with either 40 mmol/L of ATGL inhibitor atglistatin or DMSO (Vehicle) every 2 days. Left, representative plates. Right, the average of biologic triplicate determinations. Error bars, SD. The experiment was repeated twice with similar results.

    Cancer Res, 2016, 76(5):1204-13.. Atglistatin purchased from Selleck.

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Choose Selective Lipase Inhibitors

Biological Activity

Description Atglistatin is a highly potent, and selective inhibitor of adipose triglyceride lipase (ATGL) with IC50 of 0.7 μM, high selectivity over other key metabolic lipases.
Targets
ATGL [1]
(Cell-free assay)
0.7 μM
In vitro

Atglistatin inhibits lipolysis in cell and organ cultures by targeting ATGL with no cytotoxicity up to a concentration of 50 μM. [1]

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. [1]

Protocol

Kinase Assay:[1]
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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.
Cell Research:[1]
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  • Cell lines: AML-12 mouse hepatocytes
  • Concentrations: ~50 μM
  • Incubation Time: 2 hours
  • Method: 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)
Animal Research:[1]
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  • Animal Models: Mice (C57Bl/6J)
  • Formulation: Olive oil (oral gavage), PBS containing 0.25% Cremophor EL (i.p.)
  • Dosages: 1.4 mg/mouse (oral gavage); ~400 μmol/kg (i.p.)
  • Administration: oral gavage or i.p.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 56 mg/mL (197.62 mM)
Ethanol 4 mg/mL (14.11 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 283.37
Formula

C17H21N3O

CAS No. 1469924-27-3
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID