IAXO-102 是 TLR4 的拮抗剂，抑制 TLR4 信号通路。IAXO-102 抑制 MAPK 和 p65 NF-kB 的磷酸化及 TLR4 和 TLR4 依赖性的炎性蛋白的表达。IAXO-102 抑制实验性腹主动脉瘤的发展。
货号:ajcx39440
CAS:1115270-63-7
分子式:C35H71NO5
分子量：585.94
溶解度:Ethanol : 50 mg/mL (85.33 mM; Need ultrasonic)|DMSO : 5 mg/mL (8.53 mM; Need ultrasonic)
纯度：98%
存储：Store at -20°C
库存：现货

Background:

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.

Protocol:

TLR4