Skip to Content
Merck
  • Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice.

Discovery of XEN445: a potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice.

Bioorganic & medicinal chemistry (2013-11-12)
Shaoyi Sun, Richard Dean, Qi Jia, Alla Zenova, Jing Zhong, Celene Grayson, Clark Xie, Andrea Lindgren, Pritpaul Samra, Luis Sojo, Margaret van Heek, Linus Lin, David Percival, Jian-Min Fu, Michael D Winther, Zaihui Zhang
PMID24211162
ABSTRACT

Endothelial lipase (EL) activity has been implicated in HDL metabolism and in atherosclerotic plaque development; inhibitors are proposed to be efficacious in the treatment of dyslipidemia related cardiovascular disease. We describe here the discovery of a novel class of anthranilic acids EL inhibitors. XEN445 (compound 13) was identified as a potent and selective EL inhibitor, that showed good ADME and PK properties, and demonstrated in vivo efficacy in raising plasma HDLc concentrations in mice.