GALA-chol
GALA-chol is a cholesterol-conjugated pH-responsive fusion peptide that can serve as a delivery adjuvant. GALA-chol enhances the endocytosis of siRNA RET/PTC1-SQ nanoparticles, inhibits cell viability, and undergoes pH-responsive charge conversion in the acidic lysosomal environment, thereby promoting lysosomal escape of small extracellular vesicle (sEV) cargo. GALA-chol anchors to the sEV membrane and maintains the structural integrity and intrinsic homing activity of sEVs. GALA-chol can be used in studies related to adjuvant delivery.
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- Formule: C170H269N35O48S
- Masse moléculaire:3603.23
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Activité biologique
Nanoparticles composed of GALA-Chol (10% proportion) and 50 nM siRNA RET/PTC1-SQ reduce the viability of BHP 10-3 SC mice and TPC-1 cells by approximately 20% at 48 h and 72 h (treatment duration: 24-72 h), and the inhibitory effect is enhanced (by approximately 50%) when combined with Lipofectamine 2000[1].
Nanoparticles composed of GALA-Chol and siRNA RET/PTC1-SQ (10% GALA-Chol; 50 nM siRNA; 24-48 h) significantly inhibit the expression of RET/PTC1 gene and protein in BHP 10-3 SC mice and TPC-1 cells at both 24 h and 48 h, whereas siRNA RET/PTC1-SQ nanoparticles without GALA-Chol exhibit no silencing activity[1].
Nanoparticles composed of GALA-Chol and siRNA RET/PTC1-SQ (10% GALA-Chol; 50 nM siRNA; 4 h) are efficiently internalized by BHP 10-3 SCmice cells, while siRNA RET/PTC1-SQ nanoparticles without GALA-Chol cannot cross the cell membrane[1].
After functional modification of sEVs derived from MCF-7 cells with GALA-chol (0-10 μM/109 sEV particles), the cytoplasmic cargo delivery efficiency to MCF-7 cells reaches the maximum at a concentration of 8 μM/109 particles; at higher concentrations, the delivery efficiency decreases due to steric hindrance interference[2].
MCF-7-derived sEVs functionalized with GALA-chol (8 μM/109 sEV particles; 0-10 h) enable efficient lysosomal escape of cargo in MCF-7 cells after 6 h of incubation, showing a significant increase in cytoplasmic cargo distribution compared with non-functionalized sEVs[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:BHP 10-3 SCmice, TPC-1 (human papillary thyroid carcinoma cell lines harboring RET/PTC1 fusion oncogene)
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Concentration:10% molar ratio of GALA-Chol relative to siRNA RET/PTC1-SQ; 50 nM siRNA concentration
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Incubation Time:24 h, 48 h, 72 h
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Result:Inhibited cell viability by ~10% at 24 h and ~20% at 48 h and 72 h compared to untreated cells.
Enhanced inhibition to ~50% when combined with Lipofectamine 2000.
Chemical Information
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Masse moléculaire 3603.23
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Formule C170H269N35O48S
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Synonyms
GALA-cholesterol
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Sequence
Ac-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-{Cys(cholesterol)}-NH2
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Sequence Shortening
Ac-WEAALAEALAEALAEHLAEALAEALEALAA-{Cys(cholesterol)}--NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Ali HM, et al. Effects of silencing the RET/PTC1 oncogene in papillary thyroid carcinoma by siRNA-squalene nanoparticles with and without fusogenic companion GALA-cholesterol. Thyroid. 2014;24(2):327-338. [Content Brief]
[2]. Kim G, et al. Enhancing Gene Delivery to Breast Cancer with Highly Efficient siRNA Loading and pH-Responsive Small Extracellular Vesicles. ACS Biomater Sci Eng. 2025;11(1):213-227. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)