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| Targets |
GALA TFA does not target a specific receptor or enzyme in the traditional sense; instead, its "target" is the endosomal membrane in the context of intracellular delivery. GALA is a pH-sensitive fusogenic peptide that undergoes a conformational change from a random coil to an α-helix at acidic pH (pH 5.0-6.0), which is the pH range found in endosomes. This conformational change allows GALA to insert into and destabilize the endosomal membrane, facilitating the release of its cargo (e.g., DNA, RNA, proteins, or small molecules) from endosomes into the cytoplasm. By promoting endosomal escape, GALA enhances the efficiency of intracellular delivery and the expression of delivered genes or proteins. The peptide is not a pharmacological agent with a specific molecular target but rather a tool for improving the delivery of therapeutics and research reagents into cells.
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| ln Vitro |
In vitro, GALA TFA enhances the transfection efficiency of cationic liposomes and other delivery systems. The peptide's pH-sensitive fusogenic activity allows it to promote endosomal escape, a critical step in intracellular delivery that is often a bottleneck for efficient gene and protein delivery. When GALA is co-administered with cargo (e.g., plasmid DNA, siRNA, or proteins) and a delivery vehicle (e.g., cationic liposomes), it enhances the release of cargo from endosomes into the cytoplasm, leading to increased expression or activity of the cargo. The peptide's activity can be assessed in cell-based assays by measuring the transfection efficiency (e.g., reporter gene expression) or protein delivery efficiency (e.g., intracellular protein levels) in the presence and absence of GALA. The peptide's effectiveness depends on its ability to respond to the acidic pH of endosomes and to destabilize the endosomal membrane without causing significant cytotoxicity.
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| ln Vivo |
In vivo activity of GALA TFA has not been extensively reported in the available literature. As a delivery enhancer, the peptide could potentially be used in vivo to improve the delivery of nucleic acids or proteins to target tissues. However, specific animal model studies, dosing regimens, and quantitative outcomes have not been reported. The peptide's pH-sensitive fusogenic activity would be expected to enhance endosomal escape in vivo, improving the efficacy of gene therapy or protein therapeutics. However, challenges such as stability in biological fluids, immunogenicity, and off-target effects would need to be addressed. The peptide is primarily used as a research tool for in vitro studies of intracellular delivery. Further in vivo studies would be required to assess its potential for therapeutic applications.
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| Enzyme Assay |
In vitro enzyme or receptor binding assay protocols are not applicable to GALA TFA, as the peptide is a fusogenic peptide rather than an enzyme inhibitor or receptor ligand. However, its activity can be assessed using liposome leakage assays or cell-based delivery assays. A standard protocol for assessing GALA's fusogenic activity would involve preparing liposomes (e.g., phospholipid vesicles) containing a fluorescent dye (e.g., calcein) at self-quenching concentrations. GALA is added to the liposome suspension at varying concentrations (typically 0.1-10 μM) and at acidic pH (e.g., pH 5.0) to induce fusion and leakage of the dye, resulting in an increase in fluorescence. The pH-dependent activity of GALA can be compared at different pH values (e.g., pH 5.0, 6.0, 7.4). Alternatively, the peptide's ability to promote endosomal escape in cells can be assessed using delivery assays (see below). These assays are used to characterize the peptide's membrane-destabilizing properties.
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| Cell Assay |
In vitro cell-based assay protocols for GALA TFA typically involve assessing its ability to enhance the delivery and expression of cargo in cultured cells. A standard protocol would involve preparing lipoplexes or polyplexes containing a reporter plasmid (e.g., luciferase or GFP) and GALA, with or without a cationic lipid or polymer carrier. Cells are seeded in multi-well plates and treated with the delivery complexes for a defined period (e.g., 4-6 hours), after which the medium is replaced with fresh medium. After 24-48 hours, reporter gene expression (e.g., luciferase activity or GFP fluorescence) is measured. The enhancement of transfection efficiency by GALA is calculated by comparing expression levels in the presence and absence of GALA. For protein delivery, cells are treated with GALA and a fluorescently labeled protein, and intracellular protein levels are assessed by flow cytometry or fluorescence microscopy. Cell viability should be assessed using MTT or similar assays to ensure that the peptide does not cause significant cytotoxicity. Appropriate controls include cells treated with delivery complexes without GALA and cells treated with GALA alone.
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| Animal Protocol |
In vivo animal experimental protocols for GALA TFA have not been extensively reported. Based on its function as a delivery enhancer, potential studies might involve administering GALA with nucleic acid or protein therapeutics in animal models of disease. A hypothetical protocol for gene therapy applications would involve formulating plasmid DNA or siRNA with a delivery vehicle and GALA, and administering the formulation intravenously, intratumorally, or via other routes to mice. Endpoints would include assessment of transgene expression or target gene knockdown in target tissues, as well as evaluation of therapeutic efficacy. For protein delivery, GALA could be co-administered with a therapeutic protein to enhance its intracellular delivery. However, specific published protocols are not available, and the peptide is primarily used as a research tool for in vitro studies.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of GALA TFA have not been characterized, as the compound is a research-grade peptide used for in vitro delivery studies rather than a drug. The peptide has a molecular weight of approximately 3032.36 (free base), which is relatively large for oral bioavailability. As a peptide, it would be susceptible to proteolytic degradation and would have limited oral bioavailability. If administered parenterally, it would likely be cleared rapidly through proteolysis and renal excretion. The TFA salt form enhances solubility for formulation purposes. Specific PK parameters such as half-life, volume of distribution, clearance, and bioavailability have not been reported. The compound is not intended for in vivo administration as a therapeutic agent.
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| Toxicity/Toxicokinetics |
Toxicological data for GALA TFA are limited, as the compound is intended for research use only and has not undergone systematic toxicity testing. No acute toxicity (LD50), subchronic toxicity, genotoxicity, or reproductive toxicity studies have been reported specifically for this compound. As with all research chemicals, appropriate safety precautions should be taken when handling the compound, including working in a fume hood, wearing appropriate personal protective equipment, and avoiding inhalation, ingestion, or skin contact. The compound is not intended for human use. Researchers should consult the material safety data sheet (MSDS) for specific safety information and handling recommendations.
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| References | |
| Additional Infomation |
GALA TFA is a research-grade bioactive peptide that functions as a pH-sensitive fusogenic peptide. It undergoes a conformational change at acidic pH, facilitating fusion with lipid membranes and enhancing endosomal escape of cargo. GALA is used to improve the transfection efficiency of cationic liposomes and other delivery systems and is a promising method to accelerate intracellular delivery and enhance the expression of desired proteins. It has not entered clinical trials and is not approved for any therapeutic indication. Its mechanism of action involves pH-dependent membrane destabilization, promoting the release of cargo from endosomes into the cytoplasm. The compound is available exclusively for research purposes and is not intended for diagnostic, therapeutic, or human applications.
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| Molecular Formula |
C136H215N33O45.XC2HF3O2
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| Molecular Weight |
3032.36 (free base)
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 :~12.5 mg/mL (with sonication (<60°C))
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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.) |
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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