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  3. Squalamine

Squalamine (MSI-1256) is an aminosterol compound with broad-spectrum antiviral activity. Squalamine makes cells less conducive to certain viral replication by altering the electrostatic interactions in the inner membrane of host cells. Squalamine also has antibacterial and antitumor activities. Squalamine has broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria, fungi and protozoa. Squalamine inhibits tumor-related angiogenesis and the growth of human breast cancer cells. Squalamine restores the function of enteric nervous system in Parkinson,s disease mouse models.

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Squalamine Chemical Structure

Squalamine Chemical Structure

CAS No. : 148717-90-2

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Based on 1 publication(s) in Google Scholar

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Description

Squalamine (MSI-1256) is an aminosterol compound with broad-spectrum antiviral activity. Squalamine makes cells less conducive to certain viral replication by altering the electrostatic interactions in the inner membrane of host cells. Squalamine also has antibacterial and antitumor activities. Squalamine has broad-spectrum antibacterial activity against Gram-negative and Gram-positive bacteria, fungi and protozoa. Squalamine inhibits tumor-related angiogenesis and the growth of human breast cancer cells. Squalamine restores the function of enteric nervous system in Parkinson,s disease mouse models[1][2][3][4][5].

In Vitro

Squalamine (0-100 μg/mL; 2 h) inhibits dengue virus (Den V2) infection in HMEC-1 cells, and dengue infection is suppressed by about 60% at 40 μg/mL and completely suppressed at 100 μg/mL[1].
Squalamine (0-20 μg/mL; 16 h) effectively inhibits the replication of human hepatitis B virus (HBV) in human primary hepatocytes[1].
Squalamine (0.16-3.2 μM; 8 days) inhibits VEGF-induced proliferation of vascular endothelial cells HUVEC in a dose-dependent manner, but has no direct inhibitory effect on the proliferation of human breast MCF-7 cancer cells[2].
Squalamine (0.001-1 μM; 1 h) blocks FAK phosphorylation in HUVECs exposed to VEGF[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: HUVEC cells
Concentration: 0.001, 0.01, 0.1 and 1 μM
Incubation Time: 1 h
Result: Inhibited the phosphorylation levels of FAK in a concentration‐dependent manner
In Vivo

Squalamine (2 mg/kg; Intraperitoneal injection; 28 days) inhibits tumor growth in xenografted mice with breast cancer [2].
Squalamine (20 mg; Single application; 0-3 days) has a decolonizing effect on S. aureus on the skin in a mouse model[3].
Squalamine (20-120 mg/kg; Oral gavage; 5 days) restores the function of the mesenteric nervous system in PD mouse models[4].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Female athymic mice aged 6 weeks old bearing breast tumor xenografts[2]
Dosage: 2 mg/kg
Administration: Intraperitoneal injection (i.p.); 28 days
Result: Significantly retarded the growth of tumors, but the combination with Trastuzumab (HY-P9907) was more effective.
Suppressed MCF-7/HER-2 breast xenograft-associated angiogenesis.
Animal Model: 10 μL S. aureus suspension(108 cfu/mL) was applied to the female BALB/c mice skin[3]
Dosage: 20 mg
Administration: Single application; 3 days
Result: Reduced S. aureus viable cells by up to 4 log after two days compared with the control.
Animal Model: PD mice models ( hSNCAA53T mice and PrP-A53T human α-syn overexpressing transgenic mice)[4]
Dosage: 20, 40, 80, or 120 mg/kg
Administration: Oral gavage (i.g.); 5 days
Result: Effectively restored disordered colonic motility in PD mice models.
Increased colonic transit in PrP-A53T mice.
Reduced myenteric intrinsic primary afferent neuron excitability in hSNCAA53T mice.
Clinical Trial
Molecular Weight

627.96

Formula

C34H65N3O5S

CAS No.
Appearance

Solid

Color

White to light yellow

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

Structure Classification
Initial Source
Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (159.25 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

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C2

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Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.75 mg/mL (4.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.75 mg/mL (4.38 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.75 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (27.5 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.54%

References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.5925 mL 7.9623 mL 15.9246 mL 39.8115 mL
5 mM 0.3185 mL 1.5925 mL 3.1849 mL 7.9623 mL
10 mM 0.1592 mL 0.7962 mL 1.5925 mL 3.9811 mL
15 mM 0.1062 mL 0.5308 mL 1.0616 mL 2.6541 mL
20 mM 0.0796 mL 0.3981 mL 0.7962 mL 1.9906 mL
25 mM 0.0637 mL 0.3185 mL 0.6370 mL 1.5925 mL
30 mM 0.0531 mL 0.2654 mL 0.5308 mL 1.3270 mL
40 mM 0.0398 mL 0.1991 mL 0.3981 mL 0.9953 mL
50 mM 0.0318 mL 0.1592 mL 0.3185 mL 0.7962 mL
60 mM 0.0265 mL 0.1327 mL 0.2654 mL 0.6635 mL
80 mM 0.0199 mL 0.0995 mL 0.1991 mL 0.4976 mL
100 mM 0.0159 mL 0.0796 mL 0.1592 mL 0.3981 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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