| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
DMG-PEG-Mal (MW 2000) does not possess conventional biological targets. Its "targeting" concept manifests in two aspects: first, the maleimide group undergoes Michael addition reaction with molecules containing free thiol (-SH) groups (such as antibodies, peptides, proteins, and fluorescent probes) to form stable thioether bonds, enabling covalent functionalization of liposome surfaces; second, the hydrophilic shielding effect of the PEG chain reduces non-specific adsorption of serum proteins and recognition by the immune system, thereby prolonging circulation time in vivo.
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| ln Vitro |
The primary in vitro function of DMG-PEG-Mal (MW 2000) is as a surface modification material for liposomes or LNPs. Experimental evidence demonstrates that this molecule effectively inserts into lipid bilayer membranes and efficiently conjugates with thiol-containing targeting ligands via the terminal maleimide group. Studies show that DMG-PEG2000-modified LNPs exhibit good mRNA encapsulation efficiency (>90%) and low cytotoxicity. Regarding conjugation reactions, the maleimide-thiol reaction proceeds under mild conditions (room temperature, pH 6.5-7.5) with high selectivity and stable product formation.
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| ln Vivo |
The in vivo activity of DMG-PEG-Mal (MW 2000) is primarily manifested through its function in LNP formulations. Studies demonstrate that DMG-PEG2000-modified LNPs prolong circulation time, reduce anti-PEG antibody (APA) binding, and thereby improve the efficacy of repeated dosing regimens. In genome editing models, DMG-PEG2000 LNPs successfully delivered CRISPR components, achieving efficient editing of the PCSK9 gene in the liver (indels efficiency of 60-100%) and effectively reducing serum PCSK9 protein levels. However, traditional linear DMG-PEG2000 is prone to induce APA-mediated accelerated blood clearance (ABC) upon repeated administration, leading to diminished efficacy.
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| Enzyme Assay |
Conjugation Reaction Validation: Incubate DMG-PEG-Mal with thiol-containing model molecules (e.g., cysteine, reduced glutathione, or thiol-modified fluorescent dyes) in pH 6.5-7.5 buffer (e.g., PBS) at room temperature for 2-4 hours.
Product Analysis: Detect conjugation efficiency and product purity by HPLC, SDS-PAGE, or MALDI-TOF mass spectrometry.
Thiosulfate Displacement Assay: Quantify free thiol consumption before and after the reaction using Ellman's reagent (DTNB) to calculate conjugation efficiency.
PEG Chain Integrity Analysis: Analyze PEG chain degradation before and after the reaction by GPC or NMR.
Data Analysis: Calculate conjugation yield (typically >90%) and thioether bond formation rate.
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| Cell Assay |
LNP Preparation: Prepare LNPs or liposomes containing DMG-PEG-Mal (MW 2000) using microfluidics or thin-film hydration methods, with this component typically comprising 0.5-5% mol of total lipids.
Targeting Ligand Conjugation: Conjugate targeting ligands (e.g., targeting peptides, antibody fragments) via Mal-thiol reaction either post-LNP formation or during the formation process.
Cellular Uptake Assay: Incubate functionalized LNPs with target cells (e.g., cancer cells, hepatocytes) for 2-24 hours and assess uptake efficiency using fluorescent labels (DiD, FITC) or radioactive labels.
Cytotoxicity Assay: Assess the effect of DMG-PEG-Mal-modified LNPs on cell viability using MTT or CCK-8 assays to evaluate biocompatibility.
Transfection Efficiency Assessment: For nucleic acid-loaded LNPs (mRNA, siRNA), evaluate gene expression or silencing levels in target cells by fluorescence microscopy, flow cytometry, or qPCR.
Data Analysis: Compare the effects of varying PEGylation degrees and targeting ligand densities on cellular uptake and transfection efficiency.
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| Animal Protocol |
Animals & Models: Use BALB/c mice, C57BL/6 mice, or SD rats to establish tumor xenograft models, liver disease models (e.g., Fah knockout mice), or genome editing models.
LNP Preparation & Administration: Prepare DMG-PEG-Mal-modified LNPs loaded with therapeutic agents (mRNA, siRNA, CRISPR components) and administer via tail vein injection, typically at doses of 0.5-5 mg/kg (based on nucleic acid content).
Efficacy Assessment:
Tumor models: Measure tumor volume, survival
Protein replacement therapy: Detect target protein (e.g., FAH, hEPO) expression levels and liver function indicators (e.g., bilirubin)
Genome editing: Analyze target gene editing efficiency by TIDE or NGS
Immunogenicity Detection: Measure serum anti-PEG antibody (IgG, IgM) levels by ELISA to assess immune responses upon repeated dosing.
Tissue Distribution: Assess drug distribution in organs such as liver, spleen, and kidney by small animal in vivo imaging or fluorescence quantification.
Data Analysis: Compare differences in efficacy, immunogenicity, and tissue distribution between experimental and control groups.
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| ADME/Pharmacokinetics |
DMG-PEG-Mal (MW 2000) itself is a structural component of LNPs, and its pharmacokinetic behavior is primarily represented by the overall LNP. Studies show that DMG-PEG2000-modified LNPs exhibit prolonged circulation time, mainly attributed to the steric shielding effect of PEG chains that reduces protein adsorption and immune recognition. In BALB/c mice, DMG-PEG2000 LNPs have a terminal half-life of several hours to over ten hours, significantly longer than non-PEGylated liposomes. For storage, the powder is stable for 3 years at -20°C, and solutions are stable for 1 year at -80°C. Regarding solubility, DMG-PEG-Mal (MW 2000) is soluble in DMSO (≥55.5 mg/mL), ethanol (≥46.9 mg/mL), and water (≥18.67 mg/mL).
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| Toxicity/Toxicokinetics |
Available data indicate that DMG-PEG-Mal (MW 2000) exhibits generally low toxicity as an LNP component. In vitro cytotoxicity assays show that DMG-PEG2000-modified LNPs have no significant toxicity against various cell lines. However, conventional linear DMG-PEG2000 has immunogenicity concerns upon repeated administration: approximately 30-50% of healthy individuals and an even higher proportion of patients have pre-existing anti-PEG antibodies, and repeated injections can induce new anti-PEG antibody production, leading to accelerated blood clearance (ABC) effects that substantially diminish the therapeutic efficacy of subsequent doses. In Fah-/- mouse liver disease models, significant efficacy attenuation was observed upon repeated dosing of DMG-PEG2000 LNPs. Of note, DMG-PEG-Mal is for scientific research use only and is not for human use. Operationally, inhalation and skin contact should be avoided, and the maleimide group is moisture-sensitive and should be freshly prepared.
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| References | |
| Additional Infomation |
Polyethylene glycol-lipid micelles, primarily conjugates of polyethylene glycol (PEG) and distearate phosphatidylethanolamine (DSPE), i.e., PEG-DSPE, have emerged as promising drug delivery carriers, aiming to address the shortcomings in the biopharmaceutical properties of novel molecular entities. The flexibility in PEG-DSPE design and the simplicity of physical drug encapsulation make PEG-lipid micelles a versatile and efficient drug delivery carrier for cancer therapy. Studies have shown that they can overcome many limitations of poorly soluble drugs, such as poor biodistribution and targeting, low water solubility, and low oral bioavailability. Therefore, researchers are dedicated to fully exploring the potential of these delivery systems, passively encapsulating poorly soluble drugs and targeting lesion sites through enhanced permeability and retention (EPR) effects, and actively targeting delivery by linking the terminal PEG groups to targeting ligands, thereby improving delivery efficiency and tissue specificity. This article reviews the current status of polyethylene glycol-lipid micelles as delivery carriers for poorly soluble drugs, their biological significance, and recent advances in exploring their active targeting potential. In addition, this paper also describes the physical properties of polyethylene glycol-lipid micelles and their relationship with the inherent advantages and applications of polyethylene glycol-lipid micelles in drug delivery. [1]
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| Molecular Formula |
(C2H4O)NC40H70N2O8
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|---|---|
| Molecular Weight |
2000 (Average)
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| CAS # |
3101670-33-8
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| Appearance |
White to off-white solid powder
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| Synonyms |
DMG-PEG2000 Mal; DMG PEG2000-Mal
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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 |
This proudct requires strict temperature control (<8°C) during shipping.
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| Solubility (In Vitro) |
DMSO: ~100 mg/mL
Ethanol: ~100 mg/mL |
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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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