| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 500mg |
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| Other Sizes |
| Targets |
No direct biological target; the NHS ester reacts with primary amines (-NH2) to form stable amide bonds; DSPE moiety anchors into lipid bilayers for nanoparticle formulation.
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|---|---|
| ln Vitro |
DSPE-PEG-NHS (MW 3400) has no direct biological activity; it is a formulation excipient. The NHS ester reacts efficiently with primary amine groups on proteins (e.g., antibodies, targeting peptides) at pH 7.4-8.5, enabling covalent conjugation of targeting ligands to pre-formed liposomes via post-insertion.
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| ln Vivo |
No in vivo activity data for the PEG-lipid itself; DSPE-PEG-NHS is used to prepare targeted liposomes that deliver therapeutic payloads (e.g., doxorubicin, siRNA) to specific tissues, improving efficacy and reducing off-target toxicity.
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| Enzyme Assay |
Chemical conjugation efficiency is assessed by reacting NHS ester with amine-containing molecules (e.g., lysine-containing peptides or proteins). The reaction is monitored by HPLC or by measuring disappearance of primary amines using TNBSA assay or by SDS-PAGE for protein conjugation.
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| Cell Assay |
Liposomes containing DSPE-PEG-NHS are incubated with amine-functionalized targeting ligands (e.g., antibodies, folate, peptides) at pH 8.0-8.5 for 2-4 h at room temperature; unreacted NHS ester is quenched with Tris or ethanolamine; conjugation efficiency is assessed by SDS-PAGE or by measuring ligand concentration in liposome pellets.
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| Animal Protocol |
Mice bearing tumor xenografts receive DSPE-PEG-NHS-formulated targeted liposomes encapsulating therapeutic payloads via intravenous injection (0.5-5 mg lipid/kg). Biodistribution is assessed by imaging of fluorescently labeled liposomes or by measuring payload concentrations in tissues by LC-MS/MS.
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| ADME/Pharmacokinetics |
Not applicable; DSPE-PEG-NHS is a formulation component, not a therapeutic agent. PEGylation of liposomes extends circulation half-life (stealth effect) and reduces uptake by the reticuloendothelial system, improving drug pharmacokinetics.
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| Toxicity/Toxicokinetics |
No toxicity data for DSPE-PEG-NHS alone; PEGylated phospholipids have low inherent toxicity and are generally recognized as safe for use in pharmaceutical formulations. NHS esters hydrolyze in aqueous solution; the hydrolysis product (NHS) has low toxicity.
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| References |
[1]. Zhang X, Xie Y, Jin Y, Hou X, Ye L, Lou J. The effect of RMP-7 and its derivative on transporting Evans blue liposomes into the brain. Drug Deliv. 2004;11(5):301-309.
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| Additional Infomation |
DSPE-PEG-NHS (MW 3400) is a research-grade formulation excipient for liposome surface functionalization and targeted drug delivery. It is not a drug and has no clinical trial or marketing approval status. For research use only.
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| Molecular Weight |
3400(Average)
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|---|---|
| Appearance |
Typically exists as solid at room temperature
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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 |
| 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 :~5 mg/mL
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 0.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 0.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 5.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 0.5 mg/mL (Infinity mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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.