1515856-92-4 Usage
Description
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.
Uses
XEN445 is a potent and selective endothelial lipase inhibitor.
Check Digit Verification of cas no
The CAS Registry Mumber 1515856-92-4 includes 10 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 7 digits, 1,5,1,5,8,5 and 6 respectively; the second part has 2 digits, 9 and 2 respectively.
Calculate Digit Verification of CAS Registry Number 1515856-92:
(9*1)+(8*5)+(7*1)+(6*5)+(5*8)+(4*5)+(3*6)+(2*9)+(1*2)=184
184 % 10 = 4
So 1515856-92-4 is a valid CAS Registry Number.
1515856-92-4Relevant articles and documents
Discovery of XEN445: A potent and selective endothelial lipase inhibitor raises plasma HDL-cholesterol concentration in mice
Sun, Shaoyi,Dean, Richard,Jia, Qi,Zenova, Alla,Zhong, Jing,Grayson, Celene,Xie, Clark,Lindgren, Andrea,Samra, Pritpaul,Sojo, Luis,Van Heek, Margaret,Lin, Linus,Percival, David,Fu, Jian-Min,Winther, Michael D.,Zhang, Zaihui
, p. 7724 - 7734 (2013)
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.
