GALA
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GALA is a pH-responsive amphipathic peptide consisting of 30 amino acids, which acts as a lung endothelium-targeting ligand. GALA undergoes a conformational transition from random coil to α-helix in an acidic environment at pH 5.0, thereby inducing endosomal membrane destabilization and fusion. GALA-modified liposomes traverse lung endothelial cells via clathrin-dependent endocytosis and transcytosis, and specifically accumulate in the lungs after intravenous injection. GALA significantly promotes the cytosolic release of cargos carried by exosomes, plasmids and liposomes, effectively enhances gene transfection efficiency, and drives gene knockdown of functional macromolecules (such as siRNA) in alveolar epithelial cells (with no significant cytotoxicity at effective concentrations). GALA serves as a critical tool for studies on lung cancer metastasis (e.g., melanoma lung metastasis) and lung-targeted drug delivery systems.
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- Pureté: 96.20%
- CAS No.: 107658-43-5
- Formule: C136H215N33O45
- Masse moléculaire:3032.36
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Stockage:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
GALA/Chol-LPs (11-55 nmole lipids; 2-3 h) are mainly internalized by human lung microvascular endothelial cells (HMVEC-L) via the clathrin-mediated endocytosis pathway. After 3 h of incubation, 14 μM Chlorpromazine (HY-12708) inhibits its uptake by 52%[1].
When combined with exosomes not expressing CD63-GFP and Lipofectamine LTX, GALA peptide (0.5-2 μM; 37 °C; 6 h) exhibits enhanced cellular uptake efficiency and cytosolic distribution levels in HeLa cells, with 2 μM GALA increasing the cellular uptake level by approximately 12-fold[2].
When used in combination with Lipofectamine LTX, GALA peptide (2-10 μM; 37 °C; 6 h) increases the cellular uptake of CD63-GFP-expressing exosomes in HeLa cells by approximately 1.5-fold at a concentration of 2 μM, while 10 μM GALA peptide reduces the uptake efficiency[2].
When used in combination with Texas red (HY-101878)-labeled dextran-encapsulated exosomes and Lipofectamine LTX, GALA peptide (0.5-2 μM; 37 °C; 6 h) drives efficient cytosolic release of dextran in HeLa cells, with 2 μM GALA inducing cytosolic dextran signals in approximately 60% of cells[2].
Co-treatment with the GALA peptide (2 μM; 37 °C; 24 h), saporin-loaded exosomes and Lipofectamine LTX induces approximately 98% death of HeLa cells, and exerts potent cytotoxicity by enhancing the cytoplasmic delivery of saporin[2].
GALA (0.1-5.0 μM; 12-48 h) enhances Lipofectin-mediated luciferase transfection efficiency in COS-7 cells in a concentration-dependent manner. Specifically, treatment with 0.1 μM GALA for 48 h increases the transfection efficiency by 5-fold, and GALA enhances the transfection efficiency by approximately 3.5-fold at all tested time points (12, 24, 48 h)[3].
GALA (0.1-5.0 μM; 48 h) enhances the luciferase transfection efficiency mediated by Lipofectamine 2000 in COS-7 cells, with a 2-fold increase in transfection efficiency observed after treatment with 0.1 μM GALA for 48 h[3].
GALA (0.1 μM; 5 h) does not alter the cellular localization of rhodamine-labeled plasmid DNA in Lipofectin-transfected COS-7 cells, but it colocalizes with the plasmid in vesicles and exhibits diffuse cytoplasmic staining[3].
GALA (0.1 μM; 5 h) reduces cellular uptake of rhodamine-labeled plasmid DNA in COS-7 cells transfected with cationic liposomes, with the greatest reduction (approximately 19%) observed when Lipofectin is used[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:2 μM
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Incubation Time:24 h (37 °C)
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Result:Induced significant morphological changes in HeLa cells and approximately 98% cell death, as measured by WST-1 assay, when co-treated with Lipofectamine LTX and saporin-encapsulated exosomes.
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Cell Line:COS-7 simian kidney cells
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Concentration:0.1 μM (full 48 h total incubation)
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Incubation Time:48 h (total incubation)
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Result:Did not cause a substantial decrease in cell viability in Lipofectin-transfected cells, despite increasing transfection efficiency 5-fold. Allowed reduced Lipofectamine 2000 doses with diminished cytotoxicity relative to the full liposome dose control while maintaining high transfection efficiency.
GALA/Chol-MEND and GALA/PEG2000-MEND (1.5 mg siRNA/kg; i.v.; single dose) achieve significant gene silencing in mouse type I alveolar epithelial cells, reducing podoplanin mRNA expression by 29% and 24%, respectively[1].
GALA/Chol-MEND (2 mg AuNPs/kg; i.v.; single dose) crosses the mouse lung air-blood barrier, delivering gold nanoparticles to lung endothelial cells, alveolar epithelial cells, and alveolar macrophages[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (male, 6-8 weeks old, 20-25 g)[1]
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Dosage:26.4 nmol lipids/kg
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Administration:i.v.; single dose
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Result:Achieved uptake in >70% of lung endothelial cells (CD31(+)/CD45(-)).
Achieved uptake in ~30-35% of type I alveolar epithelial cells (Podoplanin(+)/EpCAM(+)/CD31(-)/CD45(-)).
Exhibited highest lung accumulation with GALA/PEG5000-LPs.
Showed highest geometric mean fluorescence intensity in type I alveolar epithelial cells with GALA/PEG2000-LPs.
Observed extravasation from lung blood vessels, with maximum extravasation for GALA/PEG5000-LPs.
Chemical Information
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CAS No. 107658-43-5
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Appearance Solid
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Masse moléculaire 3032.36
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Formule C136H215N33O45
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Color White to off-white
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Sequence
Trp-Glu-Ala-Ala-Leu-Ala-Glu-Ala-Leu-Ala-Glu-Ala-Leu-Ala-Glu-His-Leu-Ala-Glu-Ala-Leu-Ala-Glu-Ala-Leu-Glu-Ala-Leu-Ala-Ala
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Sequence Shortening
WEAALAEALAEALAEHLAEALAEALEALAA
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvant et solubilité
DMSO : 50 mg/mL (16.49 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : 14.29 mg/mL (4.71 mM; adjust pH to 9 with 1 M NaOH)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureté et documentation
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Fiche technique (287 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Santiwarangkool S, et al. A study of the endocytosis mechanism and transendothelial activity of lung-targeted GALA-modified liposomes. J Control Release. 2019;307:55-63. [Content Brief]
[2]. Nakase I, et al. Combined treatment with a pH-sensitive fusogenic peptide and cationic lipids achieves enhanced cytosolic delivery of exosomes. Sci Rep. 2015;5:10112. Published 2015 May 26. [Content Brief]
[3]. Futaki S, et al. Unique features of a pH-sensitive fusogenic peptide that improves the transfection efficiency of cationic liposomes. J Gene Med. 2005;7(11):1450-1458. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.3298 mL | 1.6489 mL | 3.2978 mL | 8.2444 mL |
| DMSO | 5 mM | 0.0660 mL | 0.3298 mL | 0.6596 mL | 1.6489 mL |
| 10 mM | 0.0330 mL | 0.1649 mL | 0.3298 mL | 0.8244 mL | |
| 15 mM | 0.0220 mL | 0.1099 mL | 0.2199 mL | 0.5496 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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