A cell-permeable prodrug of SB 201076
SB 204990 is a potent and specific inhibitor of ATP citrate lyase (ACLY) enzyme.
SB204990 (SB) is a specific inhibitor of ACLY enzyme. SB204990 treatment leads to a decrease in cytosolic Ac-CoA level and is thus expected to decrease acetylated and active β-catenin levels[1].
SB 204990, when administered orally to rats, is absorbed into the systemic circulation. When administered in the diet (0.05-0.25%, w/w) for 1 week, SB 204990 causes a dose-related decrease in plasma cholesterol (by up to 46%) and triglyceride levels (by up to 80%) in rats. SB 204990 (25 mg/kg per day) also decreases plasma cholesterol levels (by up to 23%) and triglyceride levels (by up to 38%) in the dog, preferentially decreasing low-density lipoprotein compared with high-density lipoprotein cholesterol levels[2].
参考文献:
[1]. Shares BH, et al. Active mitochondria support osteogenic differentiation by stimulating β-catenin acetylation. J Biol Chem. 2018 Oct 12;293(41):16019-16027.
[2]. Pearce NJ, et al. The role of ATP citrate-lyase in the metabolic regulation of plasma lipids. Hypolipidaemic effects of SB-204990, a lactone prodrug of the potent ATP citrate-lyase inhibitor SB-201076. Biochem J. 1998 Aug 15;334 ( Pt 1):113-9.
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