| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| Other Sizes |
Purity: ≥95%
| Targets |
DSPE phospholipid for synthesis of lipid carrier
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|---|---|
| ln Vitro |
Despite the therapeutic promise of phospholipid-based nanocarriers, a major obstacle to their widespread clinical translation is a susceptibility to fatty acid ester hydrolysis, leading to lack of quality control and inconsistencies in self-assembly formulations. Using electrospray ionization mass spectrometry fragmentation in combination with matrix-assisted laser desorption/ionization time-of-flight mass spectrometry, we have demonstrated a method to detect hydrolysis of one or both of the fatty acid esters in a PEGylated phospholipid, DSPE-PEG, in conditions commonly applied during nanocarrier production. Because such carriers are increasingly being used to deliver peptide-based therapeutics, we further investigated the hydrolysis of phospholipid esters in conditions used for solid-phase peptide synthesis and high-performance liquid chromatography of peptides. We ultimately detail a synthetic strategy to reliably produce pure phospholipid-peptide bioconjugates (peptide amphiphiles), while avoiding unintended or unnoticed hydrolyzed byproducts that could lead to polymorphic nanotherapeutics with dampened therapeutic efficacy. We believe that such an approach could help standardize phospholipid-peptide-based therapeutic development, testing, and clinical translation. [1]
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| References | |
| Additional Infomation |
This study used immunoliposomes (antibody-guided liposomes) to deliver the antitumor drug daunorubicin to the rat brain. We introduced a conjugation method that couples a thiolized antibody to an 85 nm liposome grafted with maleimide and spatially stabilized with polyethylene glycol (PEG). The antibody is then conjugated to the terminal of the PEG-conjugated liposome. No brain tissue uptake was observed of the PEG-conjugated liposomes carrying [3H]daunorubicin. However, brain targeting of the immunoliposomes carrying [3H]daunorubicin was mediated by an OX26 monoclonal antibody that targets the rat transferrin receptor and selectively accumulates in the brain microvascular endothelial cells that constitute the blood-brain barrier in vivo. Optimal brain delivery was achieved when each liposome was conjugated with 30 OX26 antibodies. Delivery saturated at higher antibody densities. Measurement of immunoliposome levels in brain tissue over 24 hours indicated accumulation of immunoliposomes in the brain. No brain targeting was observed with immunoliposomes conjugated to a mouse IgG2a isotype control antibody. In addition, plasma clearance was achieved by co-injection of free OX26-saturated immunoliposomes. Since a single liposome can carry ≥ 10,000 drug molecules, the drug loading capacity of monoclonal antibodies can be increased by up to 4 orders of magnitude using PEG-conjugated immunoliposomes. In summary, the specific targeted delivery of OX26-mediated daunorubicin to the rat brain was achieved using an immunoliposome-based drug delivery system. [1]
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| Molecular Formula |
(C2H4O)NC51H92N3O13P.H3N
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|---|---|
| Molecular Weight |
2000
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| Exact Mass |
1046.689
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| CAS # |
474922-22-0
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| Related CAS # |
DSPE-PEG2000-Mal ammonium;474922-22-0
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| PubChem CID |
163341983
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
14
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| Rotatable Bond Count |
54
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| Heavy Atom Count |
72
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| Complexity |
1460
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCCCCCCCCCCCC(=O)OCC(COP(=O)(O)OCCNC(=O)OCCOCCNC(=O)CCN1C(=O)C=CC1=O)OC(=O)CCCCCCCCCCCCCCCCC.N
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| InChi Key |
HMLYGTOVHVFLDS-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C53H96N3O14P.H3N/c1-3-5-7-9-11-13-15-17-19-21-23-25-27-29-31-33-51(60)67-45-47(70-52(61)34-32-30-28-26-24-22-20-18-16-14-12-10-8-6-4-2)46-69-71(63,64)68-42-39-55-53(62)66-44-43-65-41-38-54-48(57)37-40-56-49(58)35-36-50(56)59;/h35-36,47H,3-34,37-46H2,1-2H3,(H,54,57)(H,55,62)(H,63,64);1H3
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| Chemical Name |
azanium;2,3-di(octadecanoyloxy)propyl 2-[2-[2-[3-(2,5-dioxopyrrol-1-yl)propanoylamino]ethoxy]ethoxycarbonylamino]ethyl phosphate
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| Synonyms |
474922-22-0; DSPE-PEG2000-MAL; DSPE-PEG(2000) Maleimide; DSPE-PEG(2000)-MAL; azane;[3-[2-[2-[2-[3-(2,5-dioxopyrrol-1-yl)propanoylamino]ethoxy]ethoxycarbonylamino]ethoxy-hydroxyphosphoryl]oxy-2-octadecanoyloxypropyl] octadecanoate
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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) |
Ethanol : ~25 mg/mL
DMF : 10 mg/mL |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2 mg/mL (Infinity mM) (saturation unknown) in 10% EtOH + 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 20.0 mg/mL clear EtOH 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: ≥ 2 mg/mL (Infinity mM) (saturation unknown) in 10% EtOH + 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 20.0 mg/mL clear EtOH 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 | 0.5000 mL | 2.5000 mL | 5.0000 mL | |
| 5 mM | 0.1000 mL | 0.5000 mL | 1.0000 mL | |
| 10 mM | 0.0500 mL | 0.2500 mL | 0.5000 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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