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Etiquettes Bioactives (pour les OSAs)
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Bioactive Labels
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Position
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5’
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3’
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int
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| Cholesterol |
X
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| GalNAc |
X
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| Lipids | X |
X
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Cholesterol (Kopie)
Cholesterol is used to improve cellular uptake. By conjugating oligonucleotides to the non-toxic and hydrophobic cholesterol the oligonucleotide permeates better through the cell membrane.
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Position
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Synthesis Scale [µmol]
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Purification
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0.04
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0.2
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1.0
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15
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Des
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HPLC
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PAGE
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| 3' |
X
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X
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O |
X
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X | ||
N-acetylgalactosamine (GalNAc) (Kopie)
Conjugation of N-acetylgalactosamine (GalNAc) has become a major clinical strategy for delivery of oligonucleotides to hepatocytes (liver cells). Such conjugates are efficiently internalized by binding to the asialoglycoprotein receptor (ASGR), which exhibits high affinity for N-acetyl galactosamine terminated oligosaccharides.
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Position
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Synthesis Scale [µmol]
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Purification
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0.04
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0.2
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1.0
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15
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Des
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HPLC
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HPLC & Dialysis |
| 3' |
X
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X
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O |
X
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X | ||
Lipids (Kopie)
These modifications introduce a highly hydrophobic residue into the oligonucleotide. They are currently under investigation for oligonucleotide conjugations that could potentially help improve cell delivery and potentially increase the half-life of therapeutic oligonucleotides (ASO) in vivo.
Lauric acid (C12)
Palmitate (Palmitic Acid (C16))
Behenic Acid (C22)
Palmitoleic acid (C16:1)
Oleic Acid (C18:1)
Linoleic Acid (C18:2)
Eicosapentaenoic Acid (C20:5)
| Modification | Position | Synthesis Scale [µmol] | Purification | |||||
| 0.04 | 0.2 | 1.0 | 15 | Des | HPLC | HPLC & Dialysis | ||
| Palmitate (Palmitic acid (C16)) | 5' | O | O | O | X | X | ||
| Palmitate (Palmitic acid (C16)) | 3' | O | O | O | X | X | ||
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Lauric acid (C12) Behenic acid (C22) Palmitoleic acid (C16:1) Oleic acid (C18:1) Linoleic acid (C18:2) Eicosapentaenoic acid (C20:5) |
3' or 5' | O | O | O | O | O | ||
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Other lipids |
Please send us a request specifying your desired lipid, and we'll gladly explore how we can assist you.
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