IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. IAXO-102 inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development[1].
IAXO-102 (1-10 µM, for 2 hours) inhibits MAPK and p65 NF-κB phosphorylation in human umbilical vein endothelial (HUVEC) cells[1].IAXO-102 (10 µM, for 17 hours) suppresses LPS induced proinflammatory proteins MCP-1 and IL-8 production in HUVEC[1].
IAXO-102 (3 mg/kg/day, s.c. for 28 days) significantly retards Angiotensin II induced increase in aortic diameter in mice[1].
[1]. Huggins C, et al. A novel small molecule TLR4 antagonist (IAXO-102) negatively regulates non-hematopoietic toll like receptor 4 signalling and inhibits aortic aneurysms development. Atherosclerosis. 2015 Oct;242(2):563-70.