| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
| Targets |
None (non-receptor delivery vehicle). GL67 pentahydrochloride does not target a specific receptor but functions as a cationic lipid-based non-viral gene delivery system. Its primary mechanism involves electrostatic binding between the positively charged spermine headgroup and negatively charged phosphate backbones of nucleic acids (DNA, RNA, siRNA), forming supramolecular complexes called lipoplexes. These lipoplexes facilitate cellular uptake by interacting with the anionic cell membrane, followed by endocytosis. Once internalized, the lipoplexes may escape from endosomes via charge-mediated destabilization, allowing the nucleic acid cargo to reach the cytoplasm or nucleus for expression or silencing.
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| ln Vitro |
In vitro, GL67 pentahydrochloride demonstrates efficient nucleic acid delivery in a variety of cell lines. When complexed with plasmid DNA encoding a reporter gene (e.g., luciferase or GFP), GL67 lipoplexes transfect cells with higher efficiency than many other commercially available cationic lipids. The transfection efficiency is cell-type dependent, with highest activity observed in rapidly dividing cells and in vivo. GL67 also effectively delivers siRNA for gene silencing studies. In addition to DNA and siRNA, GL67 can deliver mRNA and CRISPR/Cas9 components for genome editing applications. The formulation parameters (e.g., lipid-to-DNA ratio, serum presence, particle size) significantly affect transfection outcomes.
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| ln Vivo |
In vivo, GL67 pentahydrochloride has been shown to be a highly effective gene delivery vehicle, particularly for pulmonary administration. Intratracheal or intranasal instillation of GL67/pDNA lipoplexes results in robust and sustained transgene expression in the lungs, making it a valuable tool for respiratory disease gene therapy and vaccine development (including COVID-19 vaccine research). Intravenous administration of GL67 lipoplexes leads to predominant expression in the lungs, with lower levels in the liver and spleen. Local administration (intramuscular, intratumoral) allows tissue-specific gene delivery. Studies in mice, rats, and larger animal models (sheep, non-human primates) confirm its in vivo transfection capabilities, though efficiency may vary by species and route of administration.
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| Enzyme Assay |
As a nucleic acid delivery vehicle, GL67 pentahydrochloride is not typically subjected to enzyme/receptor binding assays. However, its interaction with plasmid DNA can be characterized using an ethidium bromide (EtBr) displacement assay. Plasmid DNA (0.2 ug/uL) is incubated with increasing concentrations of GL67 (lipid-to-DNA charge ratios from 0.5:1 to 10:1) in 10 mM HEPES buffer (pH 7.4) for 30 minutes at room temperature. EtBr (0.4 ug/mL) is added, and fluorescence is measured at excitation 510 nm/emission 590 nm in a fluorescence plate reader. A decrease in fluorescence indicates EtBr displacement due to DNA condensation by GL67. The degree of DNA condensation (protection) is also assessed by DNase I protection assay.
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| Cell Assay |
For in vitro transfection studies, adherent cells (e.g., HEK293, HeLa, A549) are seeded in 24-well plates at 1-2 × 10^5 cells/well in growth medium without antibiotics 24 hours prior to transfection. GL67 pentahydrochloride is diluted in serum-free Opti-MEM, and plasmid DNA (0.5-1 ug/well) is added to achieve the desired charge ratio (typically 1:1 to 4:1 cationic lipid:DNA ratio). The mixture is incubated for 20-30 minutes at room temperature to allow lipoplex formation. Lipoplexes are added dropwise to cells, and transfection is allowed to proceed for 4-6 hours at 37degC. The medium is then replaced with complete growth medium, and cells are incubated for an additional 24-72 hours. Transfection efficiency is determined by luciferase assay, flow cytometry (GFP expression), or qPCR. Cytotoxicity is assessed by MTT or LDH release assay to determine optimal transfection conditions.
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| Animal Protocol |
For in vivo pulmonary delivery studies, BALB/c mice (6-8 weeks old) are anesthetized by intraperitoneal injection of ketamine/xylazine. GL67 pentahydrochloride is freshly formulated with plasmid DNA (e.g., 50 ug DNA in 50 uL of 10% sucrose solution) at a 1:1 or 2:1 lipid-to-DNA charge ratio and incubated for 20 minutes at room temperature. The lipoplex solution (50 uL) is administered intranasally or intratracheally to mice using a micropipette. For intravenous administration, the lipoplex solution (100-200 uL) is injected via the tail vein. At 24, 48, or 72 hours post-administration, mice are euthanized, and tissues (lungs, liver, spleen, heart, kidneys) are harvested. Tissues are homogenized, and transgene expression (e.g., luciferase activity measured by luminometry) is quantified after normalization to total protein concentration. Alternatively, frozen tissue sections are prepared for histological detection of reporter gene expression by in situ staining (e.g., X-gal staining for lacZ or fluorescence microscopy for GFP).
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| ADME/Pharmacokinetics |
As a cationic lipid, GL67 pentahydrochloride does not exhibit conventional PK parameters. The pharmacokinetics of GL67 is typically studied using radiolabeled or fluorescently labeled GL67 or by tracking the delivery of labeled nucleic acid cargo. Following intravenous administration, GL67 lipoplexes are rapidly cleared from circulation, with a plasma half-life of less than 5-10 minutes, due to uptake by the reticuloendothelial system (RES) and lung endothelial cells. Tissue distribution studies show predominant accumulation in the lungs (up to 40-50% of injected dose), with lower accumulation in liver, spleen, and kidneys. After pulmonary administration, GL67 lipoplexes remain in the lungs for extended periods (24-72 hours). The compound undergoes metabolic degradation in lysosomes following cellular internalization. For most research applications, the persistence of the nucleic acid cargo (days to weeks) is more relevant than the fate of the lipid itself.
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| Toxicity/Toxicokinetics |
No specific toxicity data are available for GL67 pentahydrochloride. As a cationic lipid transfection reagent, GL67 is generally considered to have acceptable tolerability for in vitro and in vivo research applications. In vitro, high concentrations or excessive lipid-to-DNA ratios may cause cytotoxicity characterized by reduced cell viability, membrane disruption, and apoptosis. In vivo, especially after intravenous administration, cationic lipid-DNA complexes can induce dose-dependent inflammatory responses including elevated serum cytokines (TNF-alpha, IL-6, IL-12) and transient hepatotoxicity (elevated AST/ALT). Pulmonary administration may cause transient mild inflammation in the airways. However, GL67 is among the less toxic cationic lipids, making it suitable for in vivo gene delivery studies. No genotoxicity or carcinogenicity has been reported.
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| References | |
| Additional Infomation |
GL67 (Genzyme Lipid 67) is one of the most widely used cationic lipids for in vivo gene delivery to the lung, originally developed by Genzyme. Its structure consists of a cholesterol anchor and a spermine headgroup, which confer excellent DNA condensing ability, endosomal buffering capacity, and low cytotoxicity compared to other cationic lipids (e.g., DOTAP, Lipofectamine 2000). The pentahydrochloride salt form indicates five equivalents of HCl, resulting in a fully protonated spermine at physiological pH for optimal DNA binding. GL67 has been extensively studied in preclinical models of cystic fibrosis (delivery of CFTR cDNA), alpha-1 antitrypsin deficiency, lung cancer (delivery of tumor suppressor genes), and vaccine development. As of 2026, no GL67-based therapy has received regulatory approval, and the compound remains a research-grade transfection reagent. The product is for research use only and not for human therapeutic application.
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| Molecular Formula |
C38H75CL5N4O2
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|---|---|
| Molecular Weight |
797.29
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| Related CAS # |
GL67;179075-30-0
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| Appearance |
White to off-white solid powder
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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) |
DMSO :~5 mg/mL (~6.27 mM)
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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 | 1.2542 mL | 6.2712 mL | 12.5425 mL | |
| 5 mM | 0.2508 mL | 1.2542 mL | 2.5085 mL | |
| 10 mM | 0.1254 mL | 0.6271 mL | 1.2542 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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