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 IC50 value of 1.68 μM in a cell-based assay using modified human embryonic kidney (HEK) cells. It does not significantly affect HEK cell viability. In a model of sepsis, CAY10614 dramatically and significantly improves survival of mice given intraperitoneal LPS.
