| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
DOPE-GA does not have a defined pharmacological target; rather, it is a lipid carrier component. As a phospholipid, it can form a micelle with a hydrophobic core to contain lipophilic drugs while maintaining a hydrophilic outer portion, facilitating interaction with cell membranes. The glutaric acid modification provides a carboxyl functional group that can be used for further conjugation (e.g., to targeting ligands or PEG), enhancing targeted delivery.
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| ln Vitro |
In vitro, DOPE-GA facilitates membrane fusion and intracellular delivery of drugs or genetic material. It can be incorporated into liposomal formulations to encapsulate therapeutic agents such as siRNA, mRNA, or small-molecule drugs. The lipid improves the stability of lipid nanoparticles and enhances their cellular uptake. It is also used as a helper lipid in cationic liposome formulations to promote endosomal escape and improve transfection efficiency.
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| ln Vivo |
In vivo, DOPE-GA-containing liposomes and lipid nanoparticles demonstrate improved drug delivery and therapeutic efficacy in animal models. When formulated into LNPs, DOPE-GA-based systems protect nucleic acid cargo from degradation, prolong circulation time, and facilitate accumulation in target tissues such as the liver. Its carboxyl group allows for conjugation of targeting ligands, potentially improving site-specific delivery. These properties make DOPE-GA a useful component in preclinical gene therapy and liver disease models.
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| Enzyme Assay |
For in vitro formulation, DOPE-GA is typically combined with other lipids (e.g., cholesterol, helper lipids, cationic lipids) in organic solvents (e.g., chloroform or ethanol) at defined molar ratios (e.g., DOPE-GA : cholesterol : cationic lipid = 30:40:30). The lipid mixture is dried under nitrogen or argon to form a thin film, which is then hydrated with an aqueous buffer (e.g., PBS, pH 7.4) containing the drug or nucleic acid cargo to be encapsulated. The resulting liposomes or LNPs are extruded through polycarbonate membranes (e.g., 100 nm pore size) to achieve uniform size distribution. Particle size and polydispersity index are measured by dynamic light scattering (DLS). Encapsulation efficiency is determined by gel electrophoresis (for nucleic acids) or HPLC (for small-molecule drugs).
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| Cell Assay |
For cellular uptake assays, fluorescently labeled cargo (e.g., FAM-siRNA or FITC-dextran) is encapsulated into DOPE-GA-based LNPs. Cells (e.g., primary hepatocytes or HepG2 cells) are incubated with the LNPs for 4-24 hours. Uptake is assessed by flow cytometry or confocal microscopy. Gene silencing efficiency is evaluated by qPCR or Western blot for the target gene. Cytotoxicity is assessed by MTT assay.
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| Animal Protocol |
For in vivo studies, DOPE-GA-based LNPs are typically formulated in a suitable vehicle such as PBS or 10% sucrose solution. The LNPs are administered via intravenous injection (tail vein) or intraperitoneal injection to rodents at doses based on the encapsulated cargo (e.g., 0.5-5 mg/kg for siRNA). Biodistribution is evaluated by measuring fluorescence (for labeled cargo) or by quantifying cargo concentration in tissues (liver, spleen, kidneys, lungs) by qPCR or HPLC. Therapeutic efficacy is assessed by measuring target gene knockdown in the liver (by qPCR/Western blot) or by monitoring disease progression in disease models (e.g., liver fibrosis, hepatocellular carcinoma).
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| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for DOPE-GA itself are not available, as it is a formulation excipient rather than an active pharmaceutical ingredient. The compound has a molecular weight of 858.1 g/mol and an extremely high XLogP of 12.9, indicating high lipophilicity and poor aqueous solubility. In liposome formulations, the overall PK properties are governed by the lipid nanoparticle as a whole, including surface properties (e.g., PEGylation), size, and charge. DOPE-GA-containing LNPs typically have a half-life of minutes to hours in circulation, depending on the formulation. The compound is stable in organic solvents and should be stored at -20degC as a powder or in solution.
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| Toxicity/Toxicokinetics |
As a formulation excipient, DOPE-GA is generally considered low in toxicity at the concentrations used in lipid nanoparticle formulations (typically <10 mg/kg in animals). In vitro cell viability assays using DOPE-GA-based liposomes at therapeutic concentrations show minimal cytotoxicity (typically >80% viability at 50-100 ug/mL). In vivo, LNP formulations containing DOPE-GA are well tolerated at standard doses, with no overt organ toxicity reported in short-term studies. Comprehensive toxicology studies are formulation-dependent and not specific to DOPE-GA alone.
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| References | |
| Additional Infomation |
DOPE-GA is a research-grade lipid and is not approved for clinical use as a stand-alone compound. It is used as a component in liposome and LNP formulations for drug delivery research, particularly for nucleic acid therapeutics (siRNA, mRNA). The CAS number is 228706-30-7, and the molecular formula is C46H84NO11P. Store at -20degC, protected from moisture and light. Its carboxyl functionality distinguishes it from unmodified DOPE, enabling conjugation to targeting moieties for enhanced delivery efficiency.
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| Molecular Formula |
C46H84NO11P
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|---|---|
| Molecular Weight |
858.13
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| Exact Mass |
857.578
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| CAS # |
228706-30-7
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| Related CAS # |
DOPE-NHS;1010188-79-0
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| PubChem CID |
46907847
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| Appearance |
Colorless to light yellow ointment
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| LogP |
12.861
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
46
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| Heavy Atom Count |
59
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| Complexity |
1150
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| Defined Atom Stereocenter Count |
1
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| SMILES |
[C@H](COP(OCCNC(CCCC(=O)O)=O)(O)=O)(COC(CCCCCCC/C=C/CCCCCCCC)=O)OC(CCCCCCC/C=C/CCCCCCCC)=O
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| InChi Key |
CSYWTOSHKUIHLT-PLQHGIRQSA-N
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| InChi Code |
InChI=1S/C46H84NO11P/c1-3-5-7-9-11-13-15-17-19-21-23-25-27-29-31-36-45(51)55-40-42(41-57-59(53,54)56-39-38-47-43(48)34-33-35-44(49)50)58-46(52)37-32-30-28-26-24-22-20-18-16-14-12-10-8-6-4-2/h17-20,42H,3-16,21-41H2,1-2H3,(H,47,48)(H,49,50)(H,53,54)/b19-17-,20-18-/t42-/m1/s1
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| Chemical Name |
5-[2-[[(2R)-2,3-bis[[(Z)-octadec-9-enoyl]oxy]propoxy]-hydroxyphosphoryl]oxyethylamino]-5-oxopentanoic acid
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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 |
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 | 1.1653 mL | 5.8266 mL | 11.6532 mL | |
| 5 mM | 0.2331 mL | 1.1653 mL | 2.3306 mL | |
| 10 mM | 0.1165 mL | 0.5827 mL | 1.1653 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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