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 [1]. 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 [1]. 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 [1].

627.96

C₃₄H₆₅N₃O₅S

148717-90-2

固体

Light yellow to yellow

角鲨胺

• Terpenoids
• Triterpenes

• 海洋天然产物
• 其他海洋生物

• 动物

Squalus acanthias

Room temperature in continental US; may vary elsewhere.

DMSO 中的溶解度 : 100 mg/mL (159.25 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

• 方案 一

  请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

  Solubility: ≥ 2.75 mg/mL (4.38 mM); 澄清溶液

  此方案可获得 ≥ 2.75 mg/mL（饱和度未知）的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

  生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。

• 方案 二

  请依序添加每种溶剂： 10% DMSO    90% (20% SBE-β-CD in Saline)

  Solubility: ≥ 2.75 mg/mL (4.38 mM); 澄清溶液

  此方案可获得 ≥ 2.75 mg/mL（饱和度未知）的澄清溶液。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液 中，混合均匀。

  20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

• 方案 三

  请依序添加每种溶剂： 10% DMSO    90% Corn Oil

  Solubility: ≥ 2.75 mg/mL (4.38 mM); 澄清溶液

  此方案可获得 ≥ 2.75 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

  以 1 mL 工作液为例，取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

• [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.  [Content Brief]

  [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.  [Content Brief]

  [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.  [Content Brief]