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Bioactive Labels (for ASOs)

 
Bioactive Labels
Position
 
5’
3’
int
Cholesterol  
on request
 
GalNAc  
X
 
Palmitate X
 
 
 

Cholesterol

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.

 
Position
Synthesis Scale [µmol]
Purification
 
0.04
0.2
1.0
15
Des
HPLC
PAGE
3'  
X
X
O  
X
X
X = available/on stock
O = on request
 

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.

 
Position
Synthesis Scale [µmol]
Purification
 
0.04
0.2
1.0
15
Des
HPLC
HPLC & Dialysis
3'  
X
X
O  
X
X
X = available/on stock
O = on request
 

Palmitate

5' 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
X = available/on stock
O = on request