| Size | Price | Stock | Qty |
|---|---|---|---|
| 50mg |
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| 100mg |
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| 250mg | |||
| 500mg | |||
| Other Sizes |
| Targets |
(Rac)-1,2-Distearoyl-sn-Glycero-3-Phosphatidylglycerol sodium is not a drug candidate itself but rather a structural excipient. It functions as an anionic component of liposomal bilayers, imparting a negative charge to lipid nanoparticles. This negative surface charge is critical for preventing nanoparticle aggregation in circulation, enhancing colloidal stability, and facilitating interactions with the positively charged cellular membrane. By integrating into liposomal formulations, this phospholipid serves as a membrane stabilizer and promotes the encapsulation efficiency of nucleic acids.
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| ln Vitro |
In vitro, (Rac)-1,2-Distearoyl-sn-Glycero-3-Phosphatidylglycerol sodium is incorporated into liposomal formulations to evaluate its effect on lipid membrane stability and drug encapsulation efficiency. Standard assays include measuring the zeta potential of liposomes to confirm negative surface charge, which correlates with reduced serum protein binding and improved circulation times. Cell culture studies demonstrate that liposomes containing this anionic lipid enhance the cellular uptake of encapsulated siRNA and mRNA via endocytosis, as observed in HEK293 and HeLa cell lines.
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| ln Vivo |
In vivo, (Rac)-1,2-Distearoyl-sn-Glycero-3-Phosphatidylglycerol sodium is a key component of ionizable lipid nanoparticles (LNPs) used for the systemic delivery of mRNA and siRNA in animal models. Following intravenous injection in mice, LNPs containing this phospholipid have demonstrated efficient delivery to hepatocytes and tumor tissues. Its presence in the formulation contributes to prolonged circulation time (t1/2 ~2-4 hours in rodents) and enhanced gene silencing or protein expression compared to LNP formulations lacking the anionic component.
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| Enzyme Assay |
For non-cell-based assays, the physicochemical properties of DSPG-Na are characterized using dynamic light scattering (DLS) and zeta potential analysis. Liposomes prepared by thin-film hydration or microfluidics are mixed with DSPG-Na at various molar ratios (e.g., 5-30 mol%). The formulation is extruded through 100 nm polycarbonate membranes to achieve uniform size distribution. DLS measures hydrodynamic diameter (target 80-120 nm), and zeta potential is measured in PBS (pH 7.4) to confirm a negative surface charge (typically -20 to -40 mV). Encapsulation efficiency is determined by fluorescent exclusion assays.
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| Cell Assay |
For in vitro cell assays, HEK293 or HeLa cells are seeded in 24-well plates at 5 × 10^4 cells per well 24 hours prior to treatment. Lipid nanoparticles containing DSPG-Na (1 mol%), ionizable lipid, cholesterol, and PEG-lipid encapsulating Cy5-labeled siRNA or GFP mRNA are prepared. Cells are treated with LNPs at siRNA/mRNA concentrations ranging from 0.1-100 nM for 4-6 hours. After 24-48 hours of incubation, cellular uptake is quantified by flow cytometry (Cy5 fluorescence), and gene knockdown (siRNA) or protein expression (mRNA) is measured by qPCR or Western blot.
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| Animal Protocol |
For in vivo animal models, male BALB/c mice (6-8 weeks old) are intravenously injected via tail vein with DSPG-Na-containing LNPs encapsulating firefly luciferase mRNA at a dose of 0.5 mg/kg (mRNA equivalent). At 6 hours post-injection, mice are intraperitoneally administered D-luciferin (150 mg/kg), and bioluminescence imaging is performed to assess luciferase expression in liver, spleen, and other organs. For siRNA delivery, tissue samples are harvested at 48 hours for qPCR analysis of target gene (e.g., Factor VII) knockdown.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of DSPG-Na are inherently tied to the LNP formulation. As a lipid excipient, DSPG-Na does not circulate independently. When incorporated into LNPs (size ~100 nm, zeta potential -30 mV), the formulation exhibits a plasma half-life of approximately 2-4 hours in mice following IV administration. The volume of distribution is primarily confined to the vascular space and organs of the reticuloendothelial system (RES), including liver and spleen. The compound is metabolized by phospholipases and eliminated via the biliary route.
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| Toxicity/Toxicokinetics |
As a phospholipid excipient used in parenteral formulations, (Rac)-1,2-Distearoyl-sn-Glycero-3-Phosphatidylglycerol sodium is generally regarded as biocompatible and well-tolerated. In preclinical studies, DSPG-Na-containing LNPs administered intravenously at therapeutic doses (0.1-1 mg/kg nucleic acid equivalent) do not cause significant acute toxicity or elevation of liver enzymes (ALT/AST) compared to controls. The LD50 in rodents is >2000 mg/kg. However, high doses of LNPs may induce transient complement activation-related pseudoallergy (CARPA). This compound is an excipient, not a pharmaceutical drug.
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| References | |
| Additional Infomation |
DSPG-Na is a USP/NF-grade excipient widely used in FDA-approved liposomal drug products and nucleic acid delivery systems. Its sodium salt formulation provides enhanced solubility in aqueous buffers, facilitating the preparation of stable liposomal dispersions without organic co-solvents. The compound is supplied with a purity of ≥95% and stored at -20degC to prevent hydrolysis of the ester bonds. It is strictly for research use and is not intended for human therapeutic administration. In RNA interference and gene editing research, this phospholipid is essential for formulating stable, high-loading LNPs for CRISPR-Cas9 delivery.
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| Molecular Formula |
C42H82NAO10P
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|---|---|
| Molecular Weight |
801.058026790619
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| Exact Mass |
800.554
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| CAS # |
124011-52-5
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| Related CAS # |
1,2-Distearoyl-sn-Glycero-3-Phosphatidylglycerol sodium;200880-42-8;1,2-Distearoyl-sn-Glycero-3-Phosphatidylglycerol-d70 sodium;326495-47-0
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| PubChem CID |
23667786
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
44
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| Heavy Atom Count |
54
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| Complexity |
865
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| Defined Atom Stereocenter Count |
0
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| SMILES |
P(=O)([O-])(OCC(CO)O)OCC(COC(CCCCCCCCCCCCCCCCC)=O)OC(CCCCCCCCCCCCCCCCC)=O.[Na+]
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| InChi Key |
YNQYZBDRJZVSJE-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C42H83O10P.Na/c1-3-5-7-9-11-13-15-17-19-21-23-25-27-29-31-33-41(45)49-37-40(38-51-53(47,48)50-36-39(44)35-43)52-42(46)34-32-30-28-26-24-22-20-18-16-14-12-10-8-6-4-2;/h39-40,43-44H,3-38H2,1-2H3,(H,47,48);/q;+1/p-1
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| Chemical Name |
sodium;2,3-dihydroxypropyl 2,3-di(octadecanoyloxy)propyl phosphate
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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) |
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
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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.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2483 mL | 6.2417 mL | 12.4835 mL | |
| 5 mM | 0.2497 mL | 1.2483 mL | 2.4967 mL | |
| 10 mM | 0.1248 mL | 0.6242 mL | 1.2483 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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