IAXO-102 is a glycolipid and an antagonist of toll-like receptor 4 (TLR4).1 It inhibits lipid A-induced TLR4 activation in a cell-based assay (IC50 = 5.013 ?M). IAXO-102 (10 mg/kg) reduces LPS-induced lethality in mice. It decreases angiotensin II-induced aortic expansion and rupture, as well as the incidence of abdominal aortic aneurysms, in ApoE-/- mice when administered at a dose of 3 mg/kg.2
1.Piazza, M., Rossini, C., Fiorentina, S.D., et al.Glycolipids and benzylammonium lipids as novel antisepsis agents: Synthesis and biological characterizationJ. Med. Chem.52(4)1209-1213(2009) 2.Huggins, C., Pearce, S.F., Peri, F., et al.A novel small molecule TLR4 antagonist (IAXO-102) negatively regulates non-hematopoietic toll like receptor 4 signalling and inhibits aortic aneurysms developmentAtherosclerosis242(2)5630570(2015)