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Biological Activity:
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.
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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.
Reference:
Products are for research use only. Not for human use.?
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