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DSPE-PEG-NHS

Cat No.:V44977 Purity: ≥95%
DSPE-PEG-NHS, pegylated phospholipid derivatives
DSPE-PEG-NHS
DSPE-PEG-NHS Chemical Structure CAS No.: 1445723-73-8
Product category: New3
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
50mg
100mg
250mg
500mg
Official Supplier of:
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Product Description
DSPE-PEG-NHS, pegylated phospholipid derivatives
DSPE-PEG-NHS (CAS: 1445723-73-8) is a PEGylated phospholipid derivative consisting of DSPE (1,2-distearoyl-sn-glycero-3-phosphoethanolamine), PEG (polyethylene glycol), and an NHS (N-hydroxysuccinimide) ester functional group. It is an amphiphilic molecule used for the conjugation of peptides, proteins, antibodies, or other amine-containing molecules to liposomes or nanoparticle surfaces. The NHS ester reacts specifically and rapidly with primary amines (-NH₂) under mild conditions (pH 8-10) to form stable amide bonds. This enables the creation of targeted drug delivery systems and functionalized biomaterials.
Biological Activity I Assay Protocols (From Reference)
Targets
The primary reactive target of DSPE-PEG-NHS is primary amine groups (-NH₂) on proteins, peptides, antibodies, and other biomolecules. The NHS ester group is the key reactive moiety that facilitates this conjugation. The DSPE component anchors the molecule into lipid bilayers, providing stability. The PEG component improves hydrophilicity, reduces opsonization, and enhances the solubility and biocompatibility of the conjugate. The molecule is not a drug that targets a biological receptor but a functionalized lipid used for drug delivery and bioconjugation.
ln Vitro
In vitro, DSPE-PEG-NHS is used to functionalize liposomes and nanoparticles for targeted drug delivery. The NHS ester reacts with primary amines on targeting ligands, such as antibodies or peptides, under mild conditions (pH 8-10) to form stable amide bonds. The PEG spacer provides flexibility and reduces non-specific interactions. The DSPE component anchors the conjugate into lipid bilayers, creating stable, functionalized nanocarriers. The compound is used to prepare targeted liposomes for in vitro cell uptake and efficacy studies.
ln Vivo
In vivo, DSPE-PEG-NHS is used to create targeted lipid nanoparticles (LNPs) and liposomes for drug delivery. The NHS ester allows the attachment of targeting moieties that direct the nanoparticles to specific tissues or cells. The PEG component prolongs circulation time by reducing opsonization and clearance by the reticuloendothelial system. The DSPE component provides stability to the lipid bilayer. These functionalized nanoparticles are used for the delivery of chemotherapeutics, nucleic acids, and imaging agents in various disease models.
Enzyme Assay
In vitro conjugation protocols involve incubating DSPE-PEG-NHS with amine-containing molecules in a suitable buffer at pH 8-10. The reaction is typically carried out at room temperature for several hours. The NHS ester reacts with primary amines to form stable amide bonds. The conjugation efficiency can be monitored by techniques such as gel electrophoresis or mass spectrometry. The resulting DSPE-PEG-ligand conjugate can then be incorporated into liposomes or nanoparticles by thin-film hydration or other standard methods. The compound is for research use only.
Animal Protocol
In vivo protocols involve the preparation of DSPE-PEG-NHS functionalized liposomes or nanoparticles containing a therapeutic or imaging agent. The nanoparticles are typically administered intravenously to animal models. The targeting ligands attached via the NHS ester direct the nanoparticles to specific tissues, enhancing drug accumulation and efficacy. The PEG component prolongs circulation time. The animals are then monitored for therapeutic response, biodistribution, and toxicity. The protocols are established for various disease models, including cancer and inflammatory diseases.
ADME/Pharmacokinetics
DSPE-PEG-NHS is an amphiphilic molecule with a molecular weight of approximately 927.08 for the PEG-free form, but the actual molecular weight depends on the PEG chain length. The molecule is soluble in DMSO and can be incorporated into lipid bilayers. The NHS ester is reactive towards primary amines at pH 8-10. The PEG component improves water solubility and biocompatibility. The compound should be stored as a powder at -20°C for up to 3 years or at 4°C for up to 2 years. In solvent, it is stable at -80°C for 6 months and at -20°C for 1 month.
Toxicity/Toxicokinetics
DSPE-PEG-NHS is considered relatively non-toxic as it is a biocompatible lipid-PEG conjugate. However, the NHS ester can react with primary amines on proteins, potentially causing irritation or allergic reactions. The compound is for research use only and not for human therapeutic use. It should be handled with appropriate safety precautions, including the use of personal protective equipment. The compound should be stored in a sealed container in a cool, dry place away from moisture and incompatible materials.
Additional Infomation
DSPE-PEG-NHS is also known as 1,2-distearoyl-sn-glycero-3-phosphoethanolamine-polyethylene glycol-N-hydroxysuccinimide. It is an amphiphilic molecule that combines a lipid anchor (DSPE), a hydrophilic spacer (PEG), and an activated ester (NHS). It is used for the conjugation of proteins, peptides, and antibodies to liposomes and nanoparticles. The NHS ester reacts specifically with primary amines at pH 8-10. It is supplied as a solid powder and should be stored at -20°C. It is for research use only.
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C47H74O18
Molecular Weight
927.08
CAS #
1445723-73-8
Appearance
Typically exists as solid at room temperature
HS Tariff Code
2934.99.9001
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)
Solubility Data
Solubility (In Vitro)
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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 : PEG300Tween 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).
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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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 1.0787 mL 5.3933 mL 10.7866 mL
5 mM 0.2157 mL 1.0787 mL 2.1573 mL
10 mM 0.1079 mL 0.5393 mL 1.0787 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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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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