Home Metabolism Lipase inhibitor Atglistatin For research use only.

Atglistatin

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.

Atglistatin Chemical Structure

Atglistatin Chemical Structure

CAS No. 1469924-27-3

Purity & Quality Control

Atglistatin Related Products

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
In vitro

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

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 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]
Animal Research Animal Models Mice (C57Bl/6J)
Dosages 1.4 mg/mouse (oral gavage); ~400 μmol/kg (i.p.)
Administration oral gavage or i.p.

Chemical Information & Solubility

Molecular Weight 283.37 Formula

C17H21N3O
CAS No. 1469924-27-3 SDF Download Atglistatin SDF
Smiles CN(C)C1=CC=C(C=C1)C2=CC(=CC=C2)NC(=O)N(C)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 57 mg/mL ( (201.15 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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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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