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.
CAS Number: 1469924-27-3
Molecular Weight: 283.37
Chemical Name: 3-(4'-(dimethylamino)biphenyl-3-yl)-1, 1-dimethylurea
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
Atglistatin was used at 10 μM final concentration in vitro and in cellular assays.
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.
- Mayer N, et al. Development of small-molecule inhibitors targeting adipose triglyceride lipase. (2013) Nat Chem Biol. 9(12):785-7.
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