Enhanced Cellular Uptake

Potential therapeutic oligonucleotides must permeate the cell membrane for optimal activity. The addition of lipophilic groups to an oligonucleotide would be expected to enhance cellular uptake/membrane permeation. The use of cholesteryl oligos and the consequent improvement in activity has been described. We have designed our Cholesteryl products with triethyleneglycol (TEG) spacers for maximum solubility. Vitamin E is both lipophilic and non-toxic even at high doses so would be an excellent candidate as a lipophilic carrier for oligonucleotides. Therefore, as an addition to our cholesteryl product line, we offer simple ?-tocopheryl (vitamin E) labelling. Totally synthetic ?-tocopherol is racemic at its three chiral centers and is used to prepare this product. The 5'-stearyl group may also become a favored lipophilic carrier for experimentation with synthetic oligonucleotides. A directed approach to the delivery of therapeutic oligonucleotides specifically to the liver has been to target the asialoglycoprotein receptor (ASGPR) using a suitable glycoconjugate. Indeed, ASGPR is the ideal target for delivery of therapeutic oligonucleotides to the liver since it combines tissue specificity, high expression levels and rapid internalization and turnover. The use of oligonucleotide glycoconjugates has led to significant advances in therapeutic delivery as evidenced by the work of Alnylam Pharmaceuticals and Ionis Pharmaceuticals using multivalent N-acetylgalactosamine (GalNAc) oligonucleotide conjugates.
7 Product Results
 
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  • 3'-Cholesteryl-TEG CPG
    3'-Cholesteryl-TEG CPG (20-2975)
    Catalog #: 20-2975
    Formal Name:

    1-Dimethoxytrityloxy-3-O-(N-cholesteryl-3-aminopropyl)-triethyleneglycol-glyceryl-2-O-succinoyl-long chain alkylamino-CPG

  • GalNAc C3 CPG
    GalNAc C3 CPG (20-2974)
    Catalog #: 20-2974
    Formal Name:

    (4-(Trimethoxytrityloxymethyl)-1-(6-(4-(3,4,6-O-triacetyl-2-acetylamino-2-deoxy-β-D-galactopyranosyl)butanamido)hexanoyl)piperidin-4-yl)methyl-O-succinoyl CPG

  • Stearyl Phosphoramidite
    Stearyl Phosphoramidite (10-1979)
    Catalog #: 10-1979
    Formal Name: Octadecyl-1-[(2-cyanoethyl)-(N,N-diisopropyl)]-phosphoramidite
  • α-Tocopherol-TEG Phosphoramidite
    α-Tocopherol-TEG Phosphoramidite (10-1977)
    Catalog #: 10-1977
    Formal Name: 1-Dimethoxytrityloxy-3-O-[(9-DL-α-tocopheryl)-triethyleneglycol-1-yl]-glyceryl-2-O-[(2-cyanoethyl)-(N,N,-diisopropyl)]-phosphoramidite
  • Cholesteryl-TEG Phosphoramidite
    Cholesteryl-TEG Phosphoramidite (10-1975)
    Catalog #: 10-1975  |  CAS #: 873435-29-1
    Formal Name:

    1-Dimethoxytrityloxy-3-O-(N-cholesteryl-3-aminopropyl)-triethyleneglycol-glyceryl-2-O-(2-cyanoethyl)-(N,N,-diisopropyl)-phosphoramidite

  • 5'-GalNAc C3 Phosphoramidite
    5'-GalNAc C3 Phosphoramidite (10-1974)
    Catalog #: 10-1974
    Formal Name:

    (4-(Trimethoxytrityloxymethyl)-1-(6-(4-(3,4,6-O-triacetyl-2-acetylamino-2-deoxy-β-D-galactopyranosyl)butanamido)hexanoyl)piperidin-4-yl)methyl-O-[(2-cyanoethyl)-(N,N-diisopropyl)] phosphoramidite

  • Spermine Phosphoramidite
    Spermine Phosphoramidite (10-1939)
    Catalog #: 10-1939
    Formal Name:

    N¹-[4-(4,4'-Dimethoxytrityloxy)butyl]-N¹,N4,N9,N¹²-tetrakis(trifluoroacetyl)-spermine-N¹²-butyl-4-[(2-cyanoethyl)-(N,N-diisopropyl)]-phosphoramidite

 
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