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A range of hydrophobic modified products (phosphoramidites and CPGs) used in the synthesis of oligonucleotides, including cholesterol (made from an entirely plant-derived source), tocopherol (vitamin E), and palmitate modifiers. These have been shown to have potential use in the delivery of oligonucleotides into cells. The hydrophobic nature of tocopherol has also been utilised as a means of improving the purification of ribozymes, and the purification of thiol-modified oligos with a view to improving the efficiency of a second ion-exchange purification.
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  2. 3'-Cholesterol SynBase™ CPG 1000/110
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    The introduction of hydrophobic residues into oligonucleotides with a view to improving their penetration into cells is an idea that has recently met with some success. Cholesteryl-conjugated oligonucleotides have in particular been the subject of substantial interest in antisense and other studies due to the lipophilicity and ready availability of cholesterol.

    Historically this has been done by post-synthetic conjugation of an amino-modified oligo to cholesterol chloroformate, however direct attachment during synthesis is much more convenient. For 3'-modification we offer 3'-Cholesterol SynBase™ CPG 1000/110. This product has a couple of notable advantages over existing products. It is not susceptible to 1,2-diol elimination as observed in some other supports. The product can also be used without IP restriction.

    For 5'-modification see Cholesterol Phosphoramidite.

      Pack Size Catalogue No Price Quantity
      4x0.2µmol 2394-P001 £50.00
      10x0.2µmol 2394-P002 £100.00
      4x1µmol 2394-P010 £80.00
      10x1µmol 2394-P008 £160.00
      4x0.2µmol MerMade 2394-P015 £50.00
      10x0.2µmol MerMade 2394-P016 £100.00
      4x1µmol MerMade 2394-P026 £80.00
      10x1µmol MerMade 2394-P022 £160.00
      100mg 2394-B100 £50.00
      1g 2394-C001 £300.00
     
  4. 5'-Tocopherol-CE Phosphoramidite
  5. View Product Details > An extension to our line of hydrophobic modifiers, based on Vitamin E. This is used to introduce tocopherol at the 5'-end of the oligo, either directly on the 5'-OH of the final base or in conjunction with a spacer or linker such as spacer 18 or C6 S-S thiol. The latter will enable the tocopherol to be cleaved via the disulphide bridge, for example once the oligo has been delivered to the cell. To include a C8 spacer natively use 5'-Octyl-tocopherol.
      Pack Size Catalogue No Price Quantity
      100µmol 2163-F100 £75.00
      250mg 2163-B250 £150.00
     
  6. 5'-Palmitate-C6-CE Phosphoramidite
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      Pack Size Catalogue No Price Quantity
      100µmol 2199-F100 £85.00
      250mg 2199-B250 £255.00
     
  8. 5'-Cholesterol-CE Phosphoramidite
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    This product is now manufactured from an entirely plant-derived source of cholesterol. A BSE/TSE statement can be provided by request.

    For 3'-modification see 3'-Cholesterol CPG.

      Pack Size Catalogue No Price Quantity
      100µmol 2170-F100 £75.00
      250mg 2170-B250 £150.00
     
  10. 5'-Cholesterol-TEG-CE Phosphoramidite
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    This product is manufactured from an entirely plant-derived source of cholesterol. A BSE/TSE statement can be provided by request.

      Pack Size Catalogue No Price Quantity
      100µmol 2189-F100 £85.00
      250mg 2189-B250 £225.00
     
  12. 5'-Octyl-tocopherol-CE Phosphoramidite (5'-C8-Tocopherol)
  13. View Product Details > An extension to our line of hydrophobic modifiers, based on Vitamin E. This is used to introduce tocopherol at the 5'-end of the oligo directly on the 5'-OH with a C8 spacer natively included. Incorporation of thiol C6 S-S will also enable the tocopherol to be cleaved via the disulphide bridge, for example once the oligo has been delivered to the cell. To omit the C8 spacer use 5'-Tocopherol.
      Pack Size Catalogue No Price Quantity
      100µmol 2194-F100 £85.00
      250mg 2194-B250 £225.00
     
  14. 3'-Palmitate SynBase™ CPG 1000/110
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    The introduction of hydrophobic residues into oligonucleotides with a view to improving their penetration into cells is an idea that has recently met with some success. Cholesteryl-conjugated oligonucleotides have in particular been the subject of substantial interest in antisense and other studies due to the lipophilicity and ready availability of cholesterol.

    Historically this has been done by post-synthetic conjugation of an amino-modified oligo to cholesterol chloroformate, however direct attachment during synthesis is much more convenient. For this purpose, therefore, we offer 3'-Cholesterol SynBase™ CPG 1000/110(2394).

    Of similar application, but comparatively less studied to date, is the incorporation of the palmitoyl moiety into oligonucletides. Recently, researchers synthesised an oligonucleotide conjugate with a 5'-terminal palmitoyl group attached through an amide bond. This has been used to modify GRN163, a thio-phosphoramidate oligonucleotide, to enhance the potency of telomerase inhibition.

    Using similar synthetic methodology to that of 2394, we have prepared 3'-Palmitate SynBase™ CPG 1000/110 for direct incorporation of a palmitoyl group during oligo synthesis.

      Pack Size Catalogue No Price Quantity
      4x0.2µmol 2393-P001 £50.00
      10x0.2µmol 2393-P002 £100.00
      4x1µmol 2393-P010 £80.00
      10x1µmol 2393-P008 £160.00
      100mg 2393-B100 £50.00
      1g 2393-C001 £300.00