Squalamine (MSI-1256)
(Synonyms: 角鲨胺; MSI-1256) 目录号 : GC32071
Squalamine (MSI-1256)(MSI-1256) 是一种氨基甾醇化合物，具有强大的广谱抗病毒活性。
Cas No.:148717-90-2
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
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].
[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.
| Cas No. | 148717-90-2 | SDF | |
| 别名 | 角鲨胺; MSI-1256 | ||
| Canonical SMILES | C[C@@]12[C@](C[C@@H](O)[C@]3([H])[C@]2([H])CC[C@@]4(C)[C@@]3([H])CC[C@]4([H])[C@@H](CC[C@H](C(C)C)OS(=O)(O)=O)C)([H])C[C@@H](NCCCNCCCCN)CC1 | ||
| 分子式 | C34H65N3O5S | 分子量 | 627.96 |
| 溶解度 | DMSO : 100 mg/mL (159.25 mM) | 储存条件 | Store at -20°C |
| General tips | 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 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 1.5925 mL | 7.9623 mL | 15.9246 mL |
| 5 mM | 0.3185 mL | 1.5925 mL | 3.1849 mL |
| 10 mM | 0.1592 mL | 0.7962 mL | 1.5925 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Staphylococcus aureus nasal decolonization strategies: a review
Expert Rev Anti Infect Ther 2019 May;17(5):327-340.PMID:31012332DOI:10.1080/14787210.2019.1604220.
Introduction: Staphylococcus aureus (S. aureus) infections are associated with increased morbidity, mortality and health-care costs. Persistent nasal carriage of S. aureus found in 10-30% of the general population, constitutes a risk factor for these infections. Nasal decolonization is one of the used strategies to prevent this risk in some situations. Areas covered: Mupirocin nasal ointment has been used for the nasal decolonization and prevention of staphylococcal infections in various settings like surgeries. However, rising rates of resistance to mupirocin require the development of new decolonization agents. In this review, we will discuss mupirocin, its origins, studies that proved its efficacy and the associated resistance, as well as other decolonization agents under investigation. Expert opinion: As some limitations exist to mupirocin use, further research for alternatives is encouraged. Some old approved antiseptics (chlorhexidine, povidone-iodine) or antibiotics (rifampicin, bacitracin) have been investigated for their efficacy in this indication. Other new agents (tea tree oil, retapamulin, LTX-109, XF-73, phages, lysostaphin, Squalamine analogues, etc.) are being studied. Some of them are still in preclinical phases, and others have reached clinical trials, but further research is needed. Special interest should be given to single dose decolonization strategies and to molecules that do not select resistant strains.
Innovative therapies for neovascular age-related macular degeneration
Expert Opin Pharmacother 2019 Oct;20(15):1879-1891.PMID:31298960DOI:10.1080/14656566.2019.1636031.
Introduction: Investigational anti-VEGF treatments for neovascular age-related macular degeneration (nAMD) aim to improve visual outcomes and reduce treatment burden; these include long-acting agents, combination strategies, topical agents, sustained-release, and genetic therapies. Areas covered: The authors provide a comprehensive review of investigational therapies for nAMD, focusing on therapies currently in clinical trial. Expert opinion: Long-acting anti-VEGF agents have demonstrated promising results in phase 3 studies, and include Brolucizumab, a single-chain antibody fragment, and Abicipar, a designed ankyrin repeat protein (DARPin). Other unique anti-VEGF agents in current trials include Conbercept - a fusion protein of the VEGF receptor domains, KSI-301 - an anti-VEGF antibody biopolymer conjugate, and OPT-302 - an inhibitor of VEGF-C/D. Strategies to activate the Tie-2 receptor, some in combination with VEGF inhibition, are of interest, with recent trials of Faricimab, ARP-1536, and nesvacumab. Topical anti-VEGF ± anti-PDGF agents, such as pazopanib, Squalamine lactate, regorafenib, and LHA510 have shown limited efficacy and/or have not been advanced, although PAN-90806 continues to advance with promising initial results. Sustained-release anti-VEGF treatments, to address treatment burden, include the ranibizumab Port Delivery System, GB-102, NT-503, hydrogel depot, Durasert, and ENV1305. Similarly, genetic therapies, including RGX-314 and ADVM-022, aim to provide sustained anti-VEGF expression from the retina.
Squalamine and Its Aminosterol Derivatives: Overview of Biological Effects and Mechanisms of Action of Compounds with Multiple Therapeutic Applications
Microorganisms 2022 Jun 13;10(6):1205.PMID:35744723DOI:10.3390/microorganisms10061205.
Squalamine is a natural aminosterol that has been discovered in the tissues of the dogfish shark (Squalus acanthias). Studies have previously demonstrated that this promoter compound and its derivatives exhibit potent bactericidal activity against Gram-negative, Gram-positive bacteria, and multidrug-resistant bacteria. The antibacterial activity of Squalamine was found to correlate with that of other antibiotics, such as colistin and polymyxins. Still, in the field of microbiology, evidence has shown that Squalamine and its derivatives have antifungal activity, antiprotozoa effect against a limited list of protozoa, and could exhibit antiviral activity against both RNA- and DNA-enveloped viruses. Furthermore, Squalamine and its derivatives have been identified as being antiangiogenic compounds in the case of several types of cancers and induce a potential positive effect in the case of other diseases such as experimental retinopathy and Parkinson's disease. Given the diverse effects of the Squalamine and its derivatives, in this review we provide the different advances in our understanding of the various effects of these promising molecules and try to draw up a non-exhaustive list of the different mechanisms of actions of Squalamine and its derivatives on the human organism and on different pathogens.
Squalamines in Blockade of Tumor-Associated Angiogenesis and Cancer Progression
Cancers (Basel) 2022 Oct 21;14(20):5154.PMID:36291938DOI:10.3390/cancers14205154.
Mechanisms of action of Squalamine in human vascular endothelial cells indicate that this compound attaches to cell membranes, potentially interacting with calmodulin, Na+/H+ exchanger isoform NHE3 and other signaling pathways involved in the angiogenic process. Thus, Squalamine elicits blockade of VEGF-induced endothelial tube-like formation in vitro. Further, Squalamine reduces growth of several preclinical models of human cancers in vivo and acts to stop metastatic tumor spread, actions due largely to blockade of angiogenesis induced by the tumor and tumor microenvironment. Squalamine in Phase I/II trials, alone or combined with standard care, shows promising antitumor activity with limited side-effects in patients with advanced solid cancers. Increased attention on Squalamine regulation of signaling pathways with or without combination treatments in solid malignancies deserves further study.
Anti-persister activity of Squalamine against Acinetobacter baumannii
Int J Antimicrob Agents 2019 Mar;53(3):337-342.PMID:30423343DOI:10.1016/j.ijantimicag.2018.11.004.
Squalamine is a natural polycationic aminosterol extracted from the shark Squalus acanthias. Squalamine displays remarkable efficacy against antimicrobial-resistant Gram-negative and Gram-positive bacteria. Its membranolytic activity and low cytotoxicity make Squalamine one of the most promising agents to fight nosocomial pathogens such as Acinetobacter baumannii. In the context of chronic diseases and therapeutic failures associated with this pathogen, the presence of dormant cells, i.e. persisters and viable but non-culturable cells (VBNCs), highly tolerant to antimicrobial compounds is problematic. The aim of this study was to investigate the antibacterial activity of Squalamine against this bacterial population of A. baumannii. Bacterial dormancy was induced by cold shock and nutrient starvation in the presence of high doses of either colistin, ciprofloxacin or Squalamine. Persisters and VBNCs induced by these treatments were then challenged with 100 mg/L Squalamine. The efficacy of each treatment was determined by evaluating culturability on agar medium, membrane integrity (LIVE/DEAD®BacLightTM staining) and respiratory activity (BacLightTM RedoxSensorTM CTC staining) of bacteria. A. baumannii ATCC 17978 generated persisters as well as VBNCs in the presence of high doses of ciprofloxacin but not colistin or Squalamine. Squalamine at 100 mg/L (below its haemolytic concentration) was able to kill dormant cells. Squalamine did not induce persister cell or VBNC formation in A. baumannii ATCC 17978. Interestingly, Squalamine was significantly active against this type of dormant population generated by ciprofloxacin, making it a very promising anti-persister agent.