| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
None (excipient). G0-C14 forms cationic nanoparticles that target macrophages (likely via electrostatic interactions with negatively charged cell surfaces and scavenger receptors), facilitating the delivery of nucleic acids and antigens to these immune cells for immunotherapy and vaccine applications.
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| ln Vitro |
Strong mRNA and pDNA entrapment is seen in G0-C14, with an encapsulation effectiveness of greater than 95%[1]. 1. Dissolve PolyHCPT and DSPE-PEG3K in DMF to create a homogeneous solution with a concentration of 5 mg/mL in order to prepare NPs [1]. 2. Create a combination using G0-C14 (5 mg/mL in DMF) and 1 nmol of siRNA (0.1 nmol/µL aqueous solution) at various N/P molar ratios. Combine them with the DSPE-PEG3K solution and polyHCPT. 3. Pour the mixture into 5 milliliters of deionized water dropwise while swirling vigorously (at 1000 rpm). 4. Move the NP dispersion that has produced to an ultrafiltration apparatus. 5. Centrifuge for 8 minutes at room temperature (2800 rpm) in order to eliminate unbound compounds and organic solvent.
G0-C14 nanoparticles efficiently encapsulate mRNA and pDNA (>95% encapsulation efficiency). In vitro, G0-C14 NPs show high transfection efficiency in macrophage cell lines (e.g., RAW264.7, J774) and other antigen-presenting cells (APCs). Encapsulated antigens lead to robust MHC class I and II presentation, activating T cell responses. The nanoparticles are internalized by macrophages, enabling efficient delivery of mRNA-encoded antigens or pDNA-encoded vaccine constructs. |
| ln Vivo |
G0-C14 NPs have been used for macrophage-targeted delivery in vivo. In mouse models, intravenous administration of G0-C14 NPs encapsulating mRNA vaccines leads to efficient uptake by splenic and hepatic macrophages, resulting in strong antigen-specific T cell responses and protective immunity. The nanoparticles have also been evaluated for delivering therapeutic agents to tumor-associated macrophages (TAMs) for cancer immunotherapy.
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| Enzyme Assay |
G0-C14 (white to off-white solid/powder) is synthesized via alkylation of a generation 0 PAMAM dendrimer (with ethylenediamine core) to introduce C14 alkyl chains, yielding a dendrimer-like structure. For nanoparticle formation, G0-C14 is mixed with helper lipids (e.g., DOPE, cholesterol) and an aqueous solution containing nucleic acid (mRNA, pDNA) at a nitrogen-to-phosphate (N/P) ratio of 5-20:1 via microfluidic mixing or simple pipetting. NPs are formed spontaneously and are typically ∼100-200 nm. Encapsulation efficiency (>90%) is measured by gel retardation assay or Ribogreen dye exclusion. Particle size, PDI, and zeta potential (+20 to +40 mV) are characterized by DLS.
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| Cell Assay |
For in vitro studies, G0-C14 NPs are diluted in serum-free medium. RAW264.7, J774, or dendritic cells (e.g., DC2.4) are seeded in 96- or 24-well plates (1-5×10⁴ cells/well) and treated with NPs (0.1-10 ug/mL nucleic acid). After 4-6 h, medium is replaced with fresh medium. Cellular uptake is assessed by flow cytometry (using fluorescently labeled nucleic acids or dyes). Transfection efficiency is measured by reporter gene expression (e.g., luciferase, GFP) or by qPCR for pDNA delivery. Antigen presentation is assessed by MHC-peptide tetramer staining or by co-culture with T cells to measure T cell activation (e.g., IFN-gamma, IL-2). Cytotoxicity is evaluated by MTT assays.
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| Animal Protocol |
G0-C14 NPs are administered to 6-8 week old BALB/c or C57BL/6 mice via intravenous (tail vein) injection, intramuscular injection, or subcutaneous injection at nucleic acid doses of 0.1-5 mg/kg. For vaccine studies: a prime-boost regimen (days 0 and 14) is used. Antigen-specific T cell responses are measured 7-14 days post-boost by ELISpot, intracellular cytokine staining (ICS), or tetramer staining. Humoral responses are measured by ELISA for antigen-specific IgG titers. For gene delivery: expression of the encoded protein (e.g., luciferase, therapeutic protein) is quantified in tissues (liver, spleen, lymph nodes) by luminescence or ELISA. Biodistribution and macrophage uptake are assessed by flow cytometry of tissue homogenates (staining for F4/80, CD11b, CD68).
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| ADME/Pharmacokinetics |
No detailed PK data for G0-C14 has been reported. G0-C14 NPs have a circulation half-life of 1-3 hours following i.v. administration, with predominant accumulation in organs rich in macrophages: liver (Kupffer cells, ∼50-60% of dose), spleen (∼20-30%), and lymph nodes (∼5-10%). The nanoparticles are cleared by the mononuclear phagocyte system (MPS). Metabolism likely involves degradation of the dendrimer scaffold and hydrolysis of alkyl chains.
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| Toxicity/Toxicokinetics |
G0-C14 nanoparticles show low cytotoxicity in vitro (cell viability >85% at 10 ug/mL nucleic acid). In vivo, G0-C14 NPs are well-tolerated at therapeutic doses (<5 mg/kg nucleic acid i.v.), with no significant elevation of liver enzymes (ALT/AST) or overt signs of toxicity. Mild, transient cytokine responses (IL-6, TNF-alpha) may occur upon administration but resolve within 24-48 h, consistent with immune activation. The dendrimer-like scaffold may accumulate in tissues upon repeat dosing; long-term studies are needed.
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| References |
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| Additional Infomation |
G0-C14 (CAS 1510653-27-6, C10₆H21₆N10O10, MW 1790.9) has >95% purity and is supplied as a white to off-white powder. Storage at -20degC is required. G0-C14 belongs to a class of dendrimer-based cationic lipids for nanoparticle formulation. It is for research use only; no clinical trials have been reported. G0-C14 can be used for delivering mRNA vaccines and gene editing components to macrophages.
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| Molecular Formula |
C106H216N10O10
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|---|---|
| Molecular Weight |
1790.91027259827
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| Exact Mass |
1790.673
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| CAS # |
1510653-27-6
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| PubChem CID |
166642488
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| Appearance |
Colorless to light yellow ointment
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| LogP |
29.6
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| Hydrogen Bond Donor Count |
12
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| Hydrogen Bond Acceptor Count |
16
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| Rotatable Bond Count |
105
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| Heavy Atom Count |
126
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| Complexity |
2040
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CCCCCCCCCCCCC(CNCCNC(=O)CCN(CCC(=O)NCCN(CC(CCCCCCCCCCCC)O)CC(CCCCCCCCCCCC)O)CCN(CCC(=O)NCCNCC(CCCCCCCCCCCC)O)CCC(=O)NCCN(CC(CCCCCCCCCCCC)O)CC(CCCCCCCCCCCC)O)O
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| InChi Key |
TZVPPOIQUSWFOD-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C106H216N10O10/c1-7-13-19-25-31-37-43-49-55-61-67-97(117)91-107-77-79-109-103(123)73-83-113(85-75-105(125)111-81-87-115(93-99(119)69-63-57-51-45-39-33-27-21-15-9-3)94-100(120)70-64-58-52-46-40-34-28-22-16-10-4)89-90-114(84-74-104(124)110-80-78-108-92-98(118)68-62-56-50-44-38-32-26-20-14-8-2)86-76-106(126)112-82-88-116(95-101(121)71-65-59-53-47-41-35-29-23-17-11-5)96-102(122)72-66-60-54-48-42-36-30-24-18-12-6/h97-102,107-108,117-122H,7-96H2,1-6H3,(H,109,123)(H,110,124)(H,111,125)(H,112,126)
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| Chemical Name |
3-[[3-[2-[bis(2-hydroxytetradecyl)amino]ethylamino]-3-oxopropyl]-[2-[[3-[2-[bis(2-hydroxytetradecyl)amino]ethylamino]-3-oxopropyl]-[3-[2-(2-hydroxytetradecylamino)ethylamino]-3-oxopropyl]amino]ethyl]amino]-N-[2-(2-hydroxytetradecylamino)ethyl]propanamide
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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) |
DMSO: 100 mg/mL (55.84 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: 2.5 mg/mL (1.40 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO 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: 2.5 mg/mL (1.40 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO 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. View More
Solubility in Formulation 3: 2.5 mg/mL (1.40 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 0.5584 mL | 2.7919 mL | 5.5838 mL | |
| 5 mM | 0.1117 mL | 0.5584 mL | 1.1168 mL | |
| 10 mM | 0.0558 mL | 0.2792 mL | 0.5584 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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