| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
None (excipient). DSPE-N3 provides azide groups on the surface of liposomes or LNPs, enabling bioorthogonal click chemistry conjugation with alkyne-modified targeting ligands (e.g., DBCO-, BCN-, or alkyne-antibodies, peptides, PEG). It is used for targeted drug delivery, imaging, and surface functionalization.
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| ln Vitro |
DSPE-N3 liposomes are stable and can be functionalized with targeting ligands via click chemistry. In vitro, antibody-conjugated DSPE-N3 liposomes (via SPAAC with DBCO-antibody) show increased cellular uptake and enhanced cytotoxicity in target cells. Conjugation efficiency is high (>85%), and the copper-free SPAAC reaction is biocompatible. DSPE-N3 can be incorporated into liposomes at 1-10 mol%.
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| ln Vivo |
DSPE-N3 liposomes have been evaluated for targeted drug delivery in vivo. Antibody- or peptide-targeted DSPE-N3 liposomes encapsulating chemotherapeutic agents show enhanced tumor accumulation and improved therapeutic efficacy in mouse xenograft models. The saturated DSPE acyl chains (C18:0) provide resistance to phospholipase degradation, prolonging circulation time. Click chemistry conjugation is performed on pre-formed liposomes, allowing precise control over ligand density.
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| Enzyme Assay |
DSPE-N3 (CAS 2839508-98-2, typical formula C44H₈₆N4O10P) is a white to off-white solid powder soluble in chloroform and DMSO. For liposome preparation: DSPE-N3 is mixed with other lipids (e.g., DOPC/DSPC, cholesterol, PEG2000-DSPE) in chloroform (typical molar ratio 5-10% for DSPE-N3). The mixture is dried, hydrated with buffer (PBS, pH 7.4), and extruded (50-200 nm pores) to form Azide-liposomes. For ligand conjugation (SPAAC, copper-free): DBCO-functionalized ligands (e.g., DBCO-antibody, DBCO-PEG, DBCO-peptide) are incubated with Azide-liposomes at room temperature or 37degC for 2-24 h in PBS, using a ligand:azide ratio of 1:2-1:10. Conjugation efficiency is measured by HPLC, fluorescent labeling, or by quantifying remaining azide groups using a fluorogenic azide-reactive probe (e.g., Cy3-DBCO). For CuAAC (copper-catalyzed): alkyne-modified ligands are incubated with Azide-liposomes, copper sulfate, sodium ascorbate, and THPTA ligand at room temperature for 1-2 h; excess copper is removed by chelation (EDTA).
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| Cell Assay |
For cellular uptake studies, cancer cells (e.g., SK-BR-3, MDA-MB-231) are seeded in 96- or 24-well plates (1-5×10⁴ cells/well) and treated with ligand-conjugated DSPE-N3 liposomes or non-targeted liposomes (0.1-1 mg/mL total lipid) containing a fluorescent dye (e.g., DiD, Rhodamine). After 2-24 h, cellular uptake is quantified by flow cytometry, and intracellular localization is visualized by confocal microscopy. Cytotoxicity is evaluated by MTT assays; ligand-targeted liposomes may show enhanced cytotoxicity. Conjugation stability: liposomes are incubated in serum (10-50% FBS) at 37degC for 24-48 h, and ligand density is measured by fluorescence to assess linker stability.
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| Animal Protocol |
For in vivo studies, DSPE-N3 liposomes (with ligand conjugated via SPAAC) are administered intravenously via the tail vein to 6-8 week old female BALB/c nude or C57BL/6 mice at lipid doses of 10-50 mg/kg, with encapsulated chemotherapeutics (e.g., doxorubicin 2-5 mg/kg). Tumor volume is measured every 2-3 days, and TGI is calculated. For biodistribution: mice are euthanized at 1, 4, 24, 48, 72 h; organs (liver, spleen, kidney, lung, tumor) are harvested, homogenized, and analyzed for drug content by HPLC. Pharmacodynamics are assessed by tumor immunohistochemistry (Ki67, TUNEL). For imaging: fluorescently labeled liposomes (e.g., with Cy5) are used for in vivo fluorescence imaging. DSPE-N3 is stable in circulation; the azide group does not react with endogenous biomolecules due to bioorthogonality, ensuring that conjugation occurs only when intended.
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| ADME/Pharmacokinetics |
DSPE-N3, incorporated into PEGylated liposomes (with PEG2000-DSPE), extends circulation half-life to 6-12 h. The saturated DSPE acyl chains (C18:0) increase membrane rigidity and resistance to phospholipase degradation. Azide groups are chemically inert toward biological molecules, ensuring no unwanted reactions in vivo. Liposomes are cleared primarily by the liver (∼30-50% of dose) and spleen (∼10-20%). Ligands conjugated via click chemistry (especially SPAAC with DBCO) are stable in circulation for at least 24-48 h.
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| Toxicity/Toxicokinetics |
DSPE-N3 has low toxicity. The azide group has no known toxicity at the concentrations used in liposomes (typically <10 mol%). The click chemistry reactions (CuAAC, SPAAC) used for conjugation are performed ex vivo before administration; residual copper (if using CuAAC) should be removed to avoid toxicity. In vivo, DSPE-N3 liposomes are well-tolerated at lipid doses ≤100 mg/kg. Standard PEGylated liposome safety applies: potential for CARPA, mild hepatotoxicity (transient ALT/AST elevation), and splenic accumulation. No severe toxicity has been reported.
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| References | |
| Additional Infomation |
DSPE-N3 (CAS 2839508-98-2, C44H₈₆N4O10P, MW approximately 885-900 Da) has >95% purity and is a white to off-white solid powder. Storage at -20degC under inert atmosphere is required to maintain azide integrity (avoid light, heat). Soluble in chloroform and DMSO. DSPE-N3 is a research-grade functionalized phospholipid; no clinical approvals have been reported. It is used for preparing targeted liposomes and LNPs via click chemistry, allowing conjugation of antibodies, peptides, sugars, dyes, and PEG for targeted drug delivery, imaging, and diagnostic applications.
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| Molecular Formula |
C43H83N4O9P
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|---|---|
| Molecular Weight |
831.114294290543
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| Exact Mass |
830.589
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| CAS # |
2839508-98-2
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| PubChem CID |
162130844
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| Appearance |
White to off-white solid powder
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| LogP |
16.1
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
46
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| Heavy Atom Count |
57
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| Complexity |
1060
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| Defined Atom Stereocenter Count |
1
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| SMILES |
CCCCCCCCCCCCCCCCCC(=O)OC[C@H](COP(=O)(O)OCCNC(=O)CN=[N+]=[N-])OC(=O)CCCCCCCCCCCCCCCCC
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| InChi Key |
ZIQJHLAPBLHPFF-RRHRGVEJSA-N
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| InChi Code |
InChI=1S/C43H83N4O9P/c1-3-5-7-9-11-13-15-17-19-21-23-25-27-29-31-33-42(49)53-38-40(39-55-57(51,52)54-36-35-45-41(48)37-46-47-44)56-43(50)34-32-30-28-26-24-22-20-18-16-14-12-10-8-6-4-2/h40H,3-39H2,1-2H3,(H,45,48)(H,51,52)/t40-/m1/s1
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| Chemical Name |
[(2R)-3-[2-[(2-azidoacetyl)amino]ethoxy-hydroxyphosphoryl]oxy-2-octadecanoyloxypropyl] octadecanoate
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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: 12.5 mg/mL (15.04 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 | 1.2032 mL | 6.0161 mL | 12.0321 mL | |
| 5 mM | 0.2406 mL | 1.2032 mL | 2.4064 mL | |
| 10 mM | 0.1203 mL | 0.6016 mL | 1.2032 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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