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Bioactive Labels (for ASOs)

 
Bioactive Labels
Position
 
5’
3’
int
Cholesterol  
X
 
GalNAc  
X
 
Lipids X
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
 

Lipids

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)

Lauric acid (C12)

5' Palmitate

Palmitate (Palmitic Acid (C16))

5' Behenic acid

Behenic Acid (C22)

Palmitoleic acid (C16:1)

Palmitoleic acid (C16:1)

Oleic Acid (C18:1)

Oleic Acid (C18:1)

Linoleic Acid (C18:2)

Linoleic Acid (C18:2)

Eicosapentaenoic Acid (C20:5)

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

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

Other lipids

Please send us a request specifying your desired lipid, and we'll gladly explore how we can assist you.
X = available/on stock
O = on request