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Bioactive Labels (for ASOs)
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Bioactive Labels
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Position
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||
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|
5’
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3’
|
int
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| Cholesterol |
on request
|
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| GalNAc |
X
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||
| Palmitate | X |
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Cholesterol
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
|
Synthesis Scale [µmol]
|
Purification
|
|||||
|
|
0.04
|
0.2
|
1.0
|
15
|
Des
|
HPLC
|
PAGE
|
| 3' |
X
|
X
|
O |
X
|
X | ||
N-acetylgalactosamine (GalNAc)
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
|
Synthesis Scale [µmol]
|
Purification
|
|||||
|
|
0.04
|
0.2
|
1.0
|
15
|
Des
|
HPLC
|
HPLC & Dialysis |
| 3' |
X
|
X
|
O |
X
|
X | ||
Palmitate
5' Palmitate introduces a highly hydrophobic residue into the oligonucleotide. Palmitate is currently under investigation as an oligonucleotide modification that could potentially help improve cell delivery and potentially increase the half-life of therapeutic oligonucleotides (ASO) in the body.
|
Position
|
Synthesis Scale [µmol]
|
Purification
|
|||||
|
|
0.04
|
0.2
|
1.0
|
15
|
Des
|
HPLC
|
HPLC & Dialysis |
| 5' |
X
|
X
|
X |
X
|
X | ||