| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg | |||
| Other Sizes |
| Targets |
The primary targets of Squalamine lactate are the sodium-hydrogen exchanger NHE3, VEGF signaling, and integrin expression. By inhibiting NHE3, it suppresses endothelial cell proliferation and migration. It also blocks the action of VEGF and integrin expression when bound to calmodulin, thereby inhibiting angiogenesis. This dual mechanism of action-directly inhibiting endothelial cells and blocking angiogenic signals-makes it a potent anti-angiogenic agent.
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| ln Vitro |
The effects of squalamine lactate on the cell signaling cascades that VEGF and other growth factors share are more extensive [1]. Squalamine inhibits angiogenesis by blocking the effects of VEGF and integrin expression when combined with calmodulin [2].
In vitro, Squalamine lactate inhibits angiogenesis by blocking the effects of VEGF and integrin expression when combined with calmodulin. It suppresses endothelial cell proliferation and migration by inhibiting the sodium-hydrogen exchanger NHE3. It also exhibits broad-spectrum antimicrobial activity via membrane disruption. These in vitro activities demonstrate its potential as both an anti-angiogenic and antimicrobial agent. It is a potent inhibitor of angiogenesis, which is a key process in tumor growth and neovascular AMD. |
| ln Vivo |
Administering squalamine intravitreally is ineffective; intravenous administration is necessary. Nonetheless, systemic treatment in humans and rodents has had encouraging outcomes [2].
In vivo, Squalamine lactate has been investigated as a treatment for neovascular AMD and as an antineoplastic agent. It is ineffective when administered intravitreally and therefore requires intravenous dosing. Its anti-angiogenic activity makes it a candidate for treating conditions characterized by abnormal blood vessel growth. In preclinical studies, it has shown promise in inhibiting angiogenesis, the formation of new blood vessels. It has been studied for its potential to prevent the progression of neovascular AMD. |
| Enzyme Assay |
Cell-free receptor binding assays for Squalamine lactate typically assess its binding to calmodulin. A standard protocol involves incubating calmodulin with a fluorescently labeled calmodulin-binding peptide and varying concentrations of Squalamine lactate. The displacement of the peptide is measured by fluorescence polarization. The IC50 is determined from the dose-response curve. This assay confirms its interaction with calmodulin, which is a key part of its mechanism of action in blocking VEGF and integrin expression.
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| Cell Assay |
For in vitro cellular experiments, endothelial cells (e.g., HUVECs) are cultured in appropriate media. Cells are treated with Squalamine lactate at various concentrations (typically 0.1-100 uM). Endothelial cell proliferation is measured using MTT or BrdU incorporation assays. Cell migration is assessed using a wound healing or Boyden chamber assay. Tube formation is assessed by culturing cells on Matrigel and measuring the formation of capillary-like structures. These assays define its anti-angiogenic potency.
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| Animal Protocol |
In vivo animal experiments with Squalamine lactate are typically conducted in models of neovascularization, such as the mouse model of choroidal neovascularization (CNV) for AMD, or in tumor xenograft models. A common protocol involves administering the compound via intravenous (IV) injection at various doses (e.g., 1-50 mg/kg). The extent of neovascularization is assessed by measuring the area of new blood vessel growth using fluorescein angiography or by histological analysis. In tumor models, tumor growth is monitored by caliper measurements.
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| ADME/Pharmacokinetics |
Squalamine lactate has a molecular weight of 627.98 g/mol. As a salt, it has improved aqueous solubility compared to the free base. It is administered intravenously due to poor oral bioavailability. Its pharmacokinetic profile is characterized by a short half-life and rapid clearance. It is stored as a powder at -20degC. For in vivo studies, it is formulated in a suitable vehicle for injection. Its development as a therapeutic has been investigated for both oncology and ophthalmology indications.
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| Toxicity/Toxicokinetics |
The toxicity profile of Squalamine lactate is generally favorable, as it has been investigated in clinical trials. Common side effects are mild and may include fatigue, nausea, and infusion-related reactions. Its mechanism of action as an anti-angiogenic agent may have effects on wound healing and other normal physiological processes. However, it is well-tolerated at therapeutic doses. It is for research use only and not for human therapeutic use in a research setting.
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| References | |
| Additional Infomation |
Squalamine lactate is the lactate form of squalamine, an aminosterol isolated from the tissue of the spiny shark (Squalus acanthias). Squalamine possesses anti-angiogenic properties; it inhibits the sodium-hydrogen exchanger NHE3, thereby suppressing endothelial cell proliferation and migration. Furthermore, this substance exhibits broad-spectrum antibacterial properties. (NCI04)
See also: Squalamine (note moved to). Squalamine lactate is an aminosterol isolated from the dogfish shark that acts as a potent anti-angiogenic agent. It inhibits angiogenesis by blocking the effects of VEGF and integrin expression when bound to calmodulin and by inhibiting the sodium-hydrogen exchanger NHE3. It has been studied for the treatment of neovascular AMD and as an antineoplastic agent. It is a valuable research tool for studying angiogenesis and related diseases. |
| Molecular Formula |
C37H71N3O8S
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|---|---|
| Molecular Weight |
718.0400
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| Exact Mass |
735.506
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| CAS # |
320725-47-1
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| Related CAS # |
Squalamine;148717-90-2
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| PubChem CID |
3036507
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| Appearance |
Light yellow to yellow solid powder
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| Hydrogen Bond Donor Count |
7
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
17
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| Heavy Atom Count |
49
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| Complexity |
1030
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| Defined Atom Stereocenter Count |
12
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| SMILES |
C[C@H](CC[C@H](C(C)C)OS(=O)(=O)O)[C@H]1CC[C@@H]2[C@@]1(CC[C@H]3[C@H]2[C@@H](C[C@@H]4[C@@]3(CC[C@@H](C4)NCCCNCCCCN)C)O)C.C[C@@H](C(=O)O)O
|
| InChi Key |
JMNXSNUXDHHTKQ-QVMSTPCGSA-N
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| InChi Code |
InChI=1S/C34H65N3O5S.C3H6O3/c1-23(2)31(42-43(39,40)41)12-9-24(3)27-10-11-28-32-29(14-16-34(27,28)5)33(4)15-13-26(21-25(33)22-30(32)38)37-20-8-19-36-18-7-6-17-35;1-2(4)3(5)6/h23-32,36-38H,6-22,35H2,1-5H3,(H,39,40,41);2,4H,1H3,(H,5,6)/t24-,25-,26+,27-,28+,29+,30-,31-,32+,33+,34-;2-/m10/s1
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| Chemical Name |
[(3R,6R)-6-[(3S,5R,7R,8R,9S,10S,13R,14S,17R)-3-[3-(4-aminobutylamino)propylamino]-7-hydroxy-10,13-dimethyl-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthren-17-yl]-2-methylheptan-3-yl] hydrogen sulfate;(2S)-2-hydroxypropanoic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ≥ 36.66 mg/mL (~51.06 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.3927 mL | 6.9634 mL | 13.9268 mL | |
| 5 mM | 0.2785 mL | 1.3927 mL | 2.7854 mL | |
| 10 mM | 0.1393 mL | 0.6963 mL | 1.3927 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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