| 产品描述: | Squalamine(MSI-1256) is an aminosterol compound with potent broad spectrum antiviral activity. IC50 value: Target: in vitro: squalamine can strongly displace membrane-bound cationic proteins such as Rac1, a ρ-GTPase recruited to the inner leaflet of the eukaryotic cytoplasmic membrane for the actin remodeling necessary for endocytosis. At concentrations between 20 and 60 μg/mL, squalamine has been shown to inhibit a broad array of growth factor-induced, actin-dependent responses in endothelial cells, including cell migration, cell division, and vascular tube formation in a 3D matrix. Squalamine effectively inhibited HBV replication in human primary hepatocytes when added either during the initial exposure of virus to the cells or at 24 h after infection. A similar study was performed to evaluate the effect of squalamine on the replication of HDV. Squalamine was introduced at 20 μg/mL during HDV exposure, and the effects were measured at day 7 when total RNA was extracted and assayed for HDV RNA sequences. in vivo: one time daily treatment with squalamine (15 or 30 mg/kg per d s.c.) was started beginning on day 1 or 2 after viral administration and continuing until day 8 or 9, respectively. Survival was monitored, and animals that remained alive by day 21 were considered cured. |
| 靶点: |
Bacterial;HBV;Others |
| 体内研究: |
Squalamine (2 mg/kg; 腹腔注射; 28 天) 在乳腺癌异种移植小鼠中抑制肿瘤的生长。 Squalamine (20 mg: 单次涂抹; 0-3 天) 在小鼠模型中对皮肤上的 S. aureus 具有去定植作用。 Squalamine (20-120 mg/kg; 灌胃; 5 天) 可恢复 PD 小鼠模型中肠神经系统的功能。 |
| 参考文献: |
1. Zasloff M, et al. Squalamine as a broad-spectrum systemic antiviral agent with therapeutic potential. Proc Natl Acad Sci U S A. 2011 Sep 20;108(38):15978-83. 2. Hraiech S, et al. Antibacterial efficacy of inhaled squalamine in a rat model of chronic Pseudomonas aeruginosa pneumonia. J Antimicrob Chemother. 2012 Oct;67(10):2452-8. 3. Djouhri-Bouktab L, et al. Squalamine ointment for Staphylococcus aureus skin decolonization in a mouse model. J Antimicrob Chemother. 2011 Jun;66(6):1306-10. |
| 溶解性: |
Soluble in DMSO |
| 保存条件: |
-80℃(运输条件:冰袋低温运输) |
| 配置溶液浓度参考: |
|
1mg |
5mg |
10mg |
| 1 mM |
1.592 ml |
7.962 ml |
15.925 ml |
| 5 mM |
0.318 ml |
1.592 ml |
3.185 ml |
| 10 mM |
0.159 ml |
0.796 ml |
1.592 ml |
| 50 mM |
0.032 ml |
0.159 ml |
0.318 ml |
|
| 注意: |
部分产品我司仅能提供部分信息,我司不保证所提供信息的权威性,仅供客户参考交流研究之用。 |