Atglistatin --- Adipose Triglyceride Lipase (ATGL) Inhibitor

Atglistatin is a highly potent, selective and competitive inhibitor of adipose triglyceride lipase (ATGL) with an IC50 of ~0.7 μM for inhibition of lipolysis in vitro, but no toxicity up to a concentration of 50 μM. Atglistatin inactivated ATGL in the presence or absence of the ATGL co-activator CGI-58. It does not displace ATGL from lipid droplets of adipocytes. Immunoprecipitation experiments revealed that Atglistatin does not interfere with the interaction of ATGL and CGI-58. Atglistatin inhibited TG hydrolase activity of wild-type WAT in a dose-dependent manner up to 78% in animal models. It was highly effective in inhibiting lipolysis in WAT organ cultures of wild-type mice. Dose and time-dependent inhibition of lipolysis was also observed in fasted wild-type C57Bl/6J mice. Atglistatin can serve as a very useful tool compound to study the pathophysiology and druggability of ATGL in animal models of metabolic disease and cachexia.

Product information

CAS Number: 1469924-27-3

Molecular Weight: 283.37

Formula: C17H21N3O

Chemical Name: 3-(4'-(dimethylamino)biphenyl-3-yl)-1, 1-dimethylurea

Smiles: CN(C)C1C=CC(=CC=1)C1=CC(=CC=C1)NC(=O)N(C)C

InChiKey: AWOPBSAJHCUSAS-UHFFFAOYSA-N

InChi: InChI=1S/C17H21N3O/c1-19(2)16-10-8-13(9-11-16)14-6-5-7-15(12-14)18-17(21)20(3)4/h5-12H,1-4H3,(H,18,21)

Technical Data

Appearance: Solid Power.

Purity: ≥98% (or refer to the Certificate of Analysis)

Solubility: DMSO up to 100 mM

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis

Storage Condition: Dry, dark and -20 ^oC for 1 year or refer to the Certificate of Analysis.

Shelf Life: ≥12 months if stored properly.

Stock Solution Storage: 0 - 4 ^oC for 1 month or refer to the Certificate of Analysis.

Drug Formulation: To be determined.

HS Tariff Code: 382200

How to use

In Vitro:

Atglistatin was used at 10 μM final concentration in vitro and in cellular assays.

In Vivo:

Atglistatin was administrated orally by gavage in olive oil (200 μl) or by intraperitoneal injection. For intraperitoneal administration, Atglistatin hydrochloride was generated by the addition of 25% HCl, resulting in a water-soluble compound. For intraperitoneal injection, the inhibitor was dried, excess HCl was buffered with Tris base and Atglistatin was dissolved in PBS containing 0.25% Cremophor EL (pH 7.1; Sigma Chemical Co.). Dosing concentration of Atglistatin is 200 μmol/kg.

References:

1. Mayer N, et al. Development of small-molecule inhibitors targeting adipose triglyceride lipase. (2013) Nat Chem Biol. 9(12):785-7.

Products are for research use only. Not for human use.

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