XEN445

Endothelial lipase, a member of the triglyceride lipase gene family expressed in endothelial cells, prefers phospholipid-enriched high-density lipoprotein (HDL) over triglyceride as a substrate. XEN445 is an endothelial lipase inhibitor (IC₅₀ = 237 nM) that demonstrates selectivity for endothelial lipase compared to lipoprotein and hepatic lipases (IC₅₀s = 20 and 9.5 μM, respectivley). An oral dose of 30 mg/kg XEN445 is reported to increase HDL cholesterol concentrations by 16% after three days and by 30% after nine days dosing in wild-type mice.

XEN445 is a potent and selective endothelial lipase inhibitor.

[1] SHAOYI SUN . Discovery of XEN445: A potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice[J]. Bioorganic & Medicinal Chemistry, 2013, 21 24: Pages 7724-7734. DOI: 10.1016/j.bmc.2013.10.023