IAXO-102

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Chemical Structure| 1115270-63-7 同义名 : -
CAS号 : 1115270-63-7
货号 : A1164931
分子式 : C35H71NO5
纯度 : 98%
分子量 : 585.94
MDL号 : MFCD31813901
存储条件:

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
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
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

[1]Huggins C, Pearce S, Peri F, Neumann F, Cockerill G, Pirianov G. 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. doi: 10.1016/j.atherosclerosis.2015.08.010. Epub 2015 Aug 8. PMID: 26318106.