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Lipopolysaccharide Antagonist; AM-12
Lipopolysaccharide Antagonist; AM-12 is an antagonist of LPS signaling without activating the inflammatory cascade. This Lipid A analog contains a glucopyranoside core, hydrophobic ether substituents, and an amino acid to provide an ionic character. It has been shown to be a very effective inhibitor of LPS-induced TNF-alpha production in human macrophages.
Highlights:
Endotoxins (Lipopolysaccharide or LPS) are a major component of the cell wall of gram-negative bacteria and are released from the bacteria as they are destroyed. LPS induces a strong response from normal immune systems and can lead to sepsis. LPS binds the CD14/TLR4/MD2 receptor complex, which promotes the secretion of pro-inflammatory cytokines in many cell types, but especially in macrophages. LPS is composed of three structural regions, one of which (the Lipid-A region) is largely responsible for the toxic activity.
- Blocks pro-inflammatory response to lipopolysaccharides (LPS)
- No toxicity or agonist activity observed (range of 0.2 - 40 uM tested)
- TNF-alpha inhibition (IC50) of 470 nM, the lowest reported for a monosaccharide compound
- Mimics classic Lipid A analogs, however, lacks the toxic disaccharide core