1115270-63-7
中文名稱
IAXO-102
英文名稱
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
2024/12/26 14:09:46
1115270-63-7 結(jié)構(gòu)式
基本信息
中文別名
化合物IAXO-102(2R,3R,4S,5R,6S)-2-(氨基甲基)-6-甲氧基-4,5-雙(十四烷氧基)四氫-2H-吡喃-3-醇
英文別名
IAXO-102α-D-Glucopyranoside, methyl 6-amino-6-deoxy-2,3-di-O-tetradecyl-
物理化學(xué)性質(zhì)
沸點650.2±55.0 °C(Predicted)
密度0.96±0.1 g/cm3(Predicted)
儲存條件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)
酸度系數(shù)(pKa)13.00±0.70(Predicted)
形態(tài)固體
顏色White to off-white
常見問題列表
生物活性
IAXO-102 是一種靶向MD-2和CD14共同受體的 TLR4 的拮抗劑。IAXO-102 可抑制 MAPK 和p65 NF-κB 磷酸化，并下調(diào)TLR4依賴性促炎蛋白的表達。IAXO-102 可抑制實驗性腹主動脈瘤 (AAA) 的發(fā)展。靶點
| Target | Value |
|
TLR4
() | |
|
MAPK
() | |
|
NF-κB
() |
體外研究
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. |
體內(nèi)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. |