| Description | IAXO-102 is a TLR4 antagonist that negatively regulates TLR4 signaling. It inhibits MAPK and p65 NF-κB phosphorylation and expression of TLR4 dependent proinflammatory protein. IAXO-102 also prevents experimental abdominal aortic aneurysm development. |
| In vitro | IAXO-102 (10 μM, for 17 hours) suppresses LPS induced pro-inflammatory proteins MCP-1 and IL-8 production in HUVEC. IAXO-102 (1-10 μM, for 2 hours) inhibits MAPK and p65 NF-κB phosphorylation in human umbilical vein endothelial (HUVEC) cells. |
| In vivo | IAXO-102 (3 mg/kg/day, s.c. for 28 days) significantly retards Angiotensin II-induced increase in aortic diameter in mice. |
| molecular weight | 585.94 |
| Molecular formula | C35H71NO5 |
| CAS | 1115270-63-7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year |
| Solubility | Ethanol: 45 mg/mL (76.8 mM), Sonication is recommended. DMSO: < 1 mg/mL (insoluble or slightly soluble) |
| References | 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. |