1115270-63-7
中文名称
IAXO-102
英文名称
IAXO-102
CAS
1115270-63-7
分子式
C35H71NO5
分子量
585.94
MOL 文件
1115270-63-7.mol
更新日期
2024/08/19 11:07:11
1115270-63-7 结构式
基本信息
中文别名
化合物IAXO-102(2R,3R,4S,5R,6S)-2-(氨基甲基)-6-甲氧基-4,5-双(十四烷氧基)四氢-2H-吡喃-3-醇
英文别名
IAXO-102α-D-Glucopyranoside, methyl 6-amino-6-deoxy-2,3-di-O-tetradecyl-
物理化学性质
沸点650.2±55.0 °C(Predicted)
密度0.96±0.1 g/cm3(Predicted)
储存条件Keep in dark place,Inert atmosphere,2-8°C
溶解度Ethanol : 50 mg/mL (85.33 mM; Need ultrasonic)|DMSO : 5 mg/mL (8.53 mM; Need ultrasonic)
酸度系数(pKa)13.00±0.70(Predicted)
形态固体
颜色White to off-white
常见问题列表
生物活性
IAXO-102 是一种靶向MD-2和CD14共同受体的 TLR4 的拮抗剂。IAXO-102 可抑制 MAPK 和p65 NF-κB 磷酸化，并下调TLR4依赖性促炎蛋白的表达。IAXO-102 可抑制实验性腹主动脉瘤 (AAA) 的发展。靶点
| Target | Value |
|
TLR4
() | |
|
MAPK
() | |
|
NF-κB
() |
体外研究
IAXO-102 (1-10 µM, for 2 hours) inhibits MAPK and p65 NF-κB phosphorylation in human umbilical vein endothelial (HUVEC) cells.
IAXO-102 (10 µM, for 17 hours) suppresses LPS induced proinflammatory proteins MCP-1 and IL-8 production in HUVEC.
Western Blot Analysis
| Cell Line: | Human umbilical vein endothelial (HUVEC) cells |
| Concentration: | 1-10 µM |
| Incubation Time: | Pretreatment for 1 hour and then exposed to LPS (100 ng/mL) for additional 1 hour |
| Result: | Significantly inhibited LPS-stimulated MAPK/p65nF-ΚB phosphorylation. |
体内研究
IAXO-102 (3 mg/kg/day, s.c. for 28 days) significantly retards Angiotensin II induced increase in aortic diameter in mice.
| Animal Model: | Six-monthold ApoE −/− /C57Bl6 |
| Dosage: | 3 mg/kg/day |
| Administration: | S.C. for 28 days |
| Result: | Significantly retarded Angiotensin II-induced increase in aortic diameter. |