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Atglistatin ATGL inhibitor

Cat.No.S7364

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 Lipase inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 283.37

Quality Control

Chemical Information, Storage & Stability

Molecular Weight 283.37 Formula

C17H21N3O

Storage (From the date of receipt)
CAS No. 1469924-27-3 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles CN(C)C1=CC=C(C=C1)C2=CC(=CC=C2)NC(=O)N(C)C

Solubility

In vitro
Batch:

DMSO : 57 mg/mL (201.15 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

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.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
ATGL [1]
(Cell-free assay)
0.7 μM
In vitro

This compound 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.
In vivo

In vivo, Atglistatin (i.p.) results in dose and time-dependent inhibition of lipolysis. Oral treatment of this compound 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, this chemical shows a distinct tissue distribution and primarily accumulates in liver and adipose tissue. [1]

References

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