生物活性 | |||
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描述 | The toll-like receptors (TLRs), including TLR4, have been shown to play a crucial role in vascular inflammatory diseases, such as atherosclerosis and aneurysm[1]. IAXO-102 is a TLR4 antagonist which negatively regulates TLR4 signalling. It 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 cell (HUVEC) cells and IAXO-102 (10 µM, for 17 hours) suppresses LPS induced proinflammatory proteins MCP-1 and IL-8 production in HUVEC[1]. In vivo potency of IAXO-102 was tested utilizing the Angiotensin II-driven experimental aneurysm development as an in vivo model. IAXO-102 (3 mg/kg/day, s.c. for 28 days) significantly retards Angiotensin II induced increase in aortic diameter in mice. Furthermore, the blocking effect of IAXO-102 was evident in all three regions of mouse aortas. Notably, IAXO-102 inhibits the rupture, incidence and development of experimental AAA (abdominal aortic aneurysm)[1]. |
实验方案 | |||
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1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
1.71mL 0.34mL 0.17mL |
8.53mL 1.71mL 0.85mL |
17.07mL 3.41mL 1.71mL |
参考文献 |
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