| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
None (excipient). PEG2000-DSPE localizes on the surface of LNPs and liposomes, providing a hydrophilic steric barrier that prevents opsonization and uptake by the mononuclear phagocyte system (MPS), thereby extending circulation time.
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|---|---|
| ln Vitro |
PEG2000-DSPE stabilizes LNP and liposome formulations in biological fluids. In vitro assays show that PEG2000-DSPE reduces serum-induced aggregation of LNPs in the presence of 50% fetal bovine serum, maintaining particle size integrity for up to 24 h. It minimizes nonspecific cellular uptake in vitro.
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| ln Vivo |
In vivo studies demonstrate PEG2000-DSPE significantly prolongs circulation half-life (from minutes to hours) and alters biodistribution of LNPs and liposomes. PEGylated LNPs encapsulating siRNA have been evaluated in mouse xenograft models, showing effective target gene knockdown in tumors. PEG2000-DSPE-containing liposomes encapsulating doxorubicin and quercetin reduce tumor growth in an MCF-7/adr multidrug-resistant breast cancer xenograft model.
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| Enzyme Assay |
PEG2000-DSPE is typically dissolved in chloroform or ethanol. For LNP or liposome preparation, it is mixed with other lipids (e.g., ionizable lipid, DOPC/DSPC, cholesterol) at 1-5 mol%. The lipid mixture is dried, hydrated, and extruded, or processed via microfluidic mixing for LNP formation. Particle size (50-150 nm) and surface PEG density are characterized by DLS and NMR.
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| Cell Assay |
For cell studies, PEG2000-DSPE LNPs or liposomes are diluted in serum-free medium and added to cells at 0.1-2 mg/mL total lipid for 2-24 h. Cellular uptake is assessed by fluorescently labeled lipids via flow cytometry or confocal imaging. PEG2000-DSPE reduces nonspecific uptake, which can be confirmed by comparing uptake of PEGylated versus non-PEGylated formulations. Cytotoxicity is evaluated by MTT assays.
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| Animal Protocol |
In animal studies, PEG2000-DSPE formulations (LNPs or liposomes) are administered intravenously to mice (tail vein) at doses of 0.5-10 mg lipid/kg. Blood samples are collected at serial time points (0, 0.5, 1, 2, 4, 8, 24 h) to measure liposome/LNP concentration by fluorescent labeling or encapsulated drug quantitation. Biodistribution in liver, spleen, kidney, and tumor is assessed 24-72 h post-dose by tissue homogenization and LC-MS/MS analysis.
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| ADME/Pharmacokinetics |
PEG2000-DSPE significantly improves PK properties of LNP and liposome formulations. Following i.v. administration, PEGylated LNPs have a circulation half-life of 6-24 h (compared to <1 h without PEG), with reduced accumulation in the liver (∼20-30% of dose vs. >50% without PEG). The PEGylated surface sterically stabilizes the particle, delaying clearance by Kupffer cells. PEG2000-DSPE is slowly metabolized via hydrolysis of the DSPE ester bonds and clearance of PEG chains.
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| Toxicity/Toxicokinetics |
PEG2000-DSPE is considered safe and biocompatible for in vivo use. PEGylated lipids are used in FDA-approved liposomal drugs. Potential adverse effects include complement activation-related pseudoallergy (CARPA) in a small subset of individuals, mediated by anti-PEG antibodies. High doses may cause vacuolation of phagocytic cells in the liver and spleen. No significant toxicity in standard preclinical models.
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| References | |
| Additional Infomation |
PEG2000-DSPE (CAS 247925-28-6, C4₅H₈₇NNaO11P, MW 2808.7) has >98% purity. It is supplied as a white to off-white solid powder. The PEG chain has a molecular weight of ∼2000 Da, with n ≈ 45 repeating ethylene oxide units. Storage at -20degC is required. PEG2000-DSPE is used in FDA-approved products (e.g., Onpattro, patisiran LNP) and numerous preclinical LNP formulations for siRNA and mRNA delivery.
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| Molecular Formula |
C45H88NO11P
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|---|---|
| Molecular Weight |
850.154096603394
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| Exact Mass |
872.599
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| CAS # |
247925-28-6
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| PubChem CID |
86278269
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
48
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| Heavy Atom Count |
59
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| Complexity |
994
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| Defined Atom Stereocenter Count |
1
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| SMILES |
P(O)(OC[C@H](OC(=O)CCCCCCCCCCCCCCCCC)COC(=O)CCCCCCCCCCCCCCCCC)(OCCNC(OCCOC)=O)=O
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| InChi Key |
OZAXVNORLZLEOJ-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C45H88NO11P.Na/c1-4-6-8-10-12-14-16-18-20-22-24-26-28-30-32-34-43(47)54-40-42(41-56-58(50,51)55-37-36-46-45(49)53-39-38-52-3)57-44(48)35-33-31-29-27-25-23-21-19-17-15-13-11-9-7-5-2;/h42H,4-41H2,1-3H3,(H,46,49)(H,50,51);
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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: 10 mg/mL (3.56 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (0.45 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 12.5 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: ≥ 1.25 mg/mL (0.45 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 12.5 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.1763 mL | 5.8813 mL | 11.7626 mL | |
| 5 mM | 0.2353 mL | 1.1763 mL | 2.3525 mL | |
| 10 mM | 0.1176 mL | 0.5881 mL | 1.1763 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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