Description
Lipid A is a lipid-
rich component of endotoxin, also known as lipopolysaccharide (LPS), which in turn is part of the outer membrane of Gram-
negative bacteria. Lipid A activates toll-
like receptor 4 (TLR4), initiating an immune response. CAY10614 is an antagonist of lipid A activation of TLR4, exhibiting an IC
50 value of 1.68 μM in a cell-
based assay using modified human embryonic kidney (HEK) cells.
1 It does not significantly affect HEK cell viability. In a model of sepsis, CAY10614 dramatically and significantly improves survival of mice given intraperitoneal LPS.
1
References
1. Piazza, M., Rossini, C., Fiorentina, S.D., et al.
Glycolipids and benzylammonium lipids as novel antisepsis agents: Synthesis and biological characterization J. Med. Chem. 52(4),1209-1213(2009).
