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.
1-Dimethoxytrityloxy-3-O-(N-cholesteryl-3-aminopropyl)-triethyleneglycol-glyceryl-2-O-(2-cyanoethyl)-(N,N,-diisopropyl)-phosphoramidite
10-O-[1-propyl-3-N-carbamoylcholesteryl]-triethyleneglycol-1-[(2-cyanoethyl)-(N,N-diisopropyl)]-phosphoramidite
1-Dimethoxytrityloxy-3-O-(N-cholesteryl-3-aminopropyl)-triethyleneglycol-glyceryl-2-O-succinoyl-long chain alkylamino-CPG