| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Targets |
As an excipient and drug delivery vehicle, m-PEG-C1-DSPE does not have a specific drug receptor target. Its biological activity is related to its physical-chemical properties: the DSPE lipid moiety anchors into lipid bilayers (e.g., of liposomes), while the hydrophilic PEG chain extends outward to create a steric barrier on the particle surface. This steric stabilization prevents opsonization and uptake by the reticuloendothelial system (RES), effectively “stealthing” the drug carrier and prolonging its circulation time in the bloodstream.
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| ln Vitro |
In vitro, m-PEG-C1-DSPE is used to formulate drug-loaded liposomes. When incorporated into liposomes, it reduces protein adsorption and lowers cell association compared to non-PEGylated liposomes. In one study, branched PEG-lipids conferred up to a 31-fold reduction in cell association. It does not exhibit direct cytotoxicity at typical formulation concentrations (e.g., <0.5 mg/mL) but may affect membrane fluidity. It is not an antimicrobial or anti-inflammatory agent.
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| ln Vivo |
In vivo, liposomes formulated with m-PEG-C1-DSPE show extended circulation half-life due to reduced clearance by the mononuclear phagocyte system (MPS). For example, PEGylated liposomes have dramatically increased AUC and prolonged presence in blood compared to conventional liposomes, enhancing the delivery of encapsulated drugs to target tissues like tumors via the enhanced permeability and retention (EPR) effect. The compound itself is non-toxic at typical doses, but it is not metabolized and may accumulate in the liver and spleen.
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| Enzyme Assay |
General in vitro liposome-protein binding assay: Prepare liposomes of varying compositions (e.g., with or without 5 mol% m-PEG-C1-DSPE). Incubate liposomes with fluorescently labeled proteins (e.g., fibrinogen) or serum for 1 hour at 37degC. Centrifuge the liposomes and measure protein adsorption by SDS-PAGE or Bradford assay. PEGylated liposomes will show a significant reduction in protein binding compared to non-PEGylated controls.
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| Cell Assay |
General in vitro cell uptake assay: Incubate fluorescently labeled liposomes (with or without m-PEG-C1-DSPE) with THP-1 macrophages (an MPS cell line) for 4 hours. Analyze cell-associated fluorescence by flow cytometry. Liposomes containing m-PEG-C1-DSPE will show up to 10-30 fold lower uptake by the macrophages, confirming the “stealth” property. Cytotoxicity in HepG2 cells can be assessed via MTT assay; the compound is considered biocompatible (IC50 > 1 mg/mL).
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| Animal Protocol |
General in vivo animal protocol for liposome PK: Formulate a model drug (e.g., doxorubicin) in liposomes with or without 5 mol% m-PEG-C1-DSPE. Administer the formulations to female BALB/c mice (n=4-5 per group) via a single intravenous injection (5 mg drug/kg). Collect blood at 0, 0.5, 1, 2, 4, 8, 24, 48, 72 h and measure plasma drug concentration by HPLC. PEGylated liposomes will have a significantly higher AUC (e.g., 10-20 fold) and longer plasma half-life (t½ ~24-48 h) than non-PEGylated liposomes.
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| ADME/Pharmacokinetics |
PEGylated phospholipids are not absorbed intact from the GI tract. When given intravenously as a component of a liposome, the DSPE anchor remains in the lipid bilayer, while the PEG chain is stable but not metabolized. The carrier liposome is taken up by the liver and spleen, where the phospholipids are slowly degraded by lysosomal phospholipases. The PEG polymer is not readily broken down and may accumulate in the liver, but at therapeutic doses, it is well-tolerated. The plasma half-life of the liposome is determined by the PEG density, typically 10-30 hours in rodents.
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| Toxicity/Toxicokinetics |
Toxicology of m-PEG-C1-DSPE is considered low. In a 28-day IV toxicity study in rats, the NOAEL for similar PEG-DSPE lipids is >100 mg/kg. The primary finding is vacuolation of macrophages in the spleen and liver, which is an expected physiological response to the accumulation of liposomal material. PEG polymers can induce anti-PEG antibodies in rare cases after repeated administration, but this is not a toxicity issue for a single-use research compound. It is non-genotoxic.
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| References | |
| Additional Infomation |
Appearance: white waxy solid. Molecular formula: variable, (C2H4O)nC40H₇₈NO₉P·Na. Storage: -20degC. Solubility: soluble in chloroform, methanol, and water. Other names: Methoxy-PEG-C1-DSPE sodium, PEG-DSPE. Safety: treat as a hazardous material.
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| Related CAS # |
m-PEG-DSPE sodium (MW 1000)
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| Appearance |
Solid powder
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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 : ~< 1 mg/mL (insoluble or slightly soluble)
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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.) |
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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