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2'-O-C16 U CPG
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2'-O-C16 U CPG
CPG used to add a lipophilic 2’-O-hexadecyl lipophilic modified adenosine to the 3' end of an oligonucleotide.
Key features
Show- Modification to enhance cell delivery.
- CPG has a long-chain alkylamino succinyl linker.
- The dR functionality conforms to a natural sugar-phosphate backbone.
- The 550 Å CPG is manufactured using our Next Generation native CPG process, offering optimized density and loading range to maximize full-length product (FLP) yield.
- 550 Å CPG suitable for high-yield applications such as therapeutic oligos (≤ 30mers).
- Contains a DMT functionality.
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Product information
Oligonucleotide therapeutics have the potential to treat a myriad of different diseases, however, their efficient delivery to targeted cells and organs remains challenging. Their high molecular size and anionic backbone hinder their cellular uptake. In addition, unmodified oligonucleotides are prone to endonuclease degradation, rapid elimination from the systemic circulation, and can trigger an immune response. Various delivery technologies have been developed to improve oligonucleotide cell delivery, including viral and non-viral carriers, and direct conjugation of oligonucleotides to ligand moieties, such as lipids.
While the conjugation of N-acetylgalactosamine (GalNAc) residues has proven to be a clinically validated way of delivering therapeutic oligonucleotides to the liver, extrahepatic tissue delivery remains challenging. The conjugation of long-chain fatty acids and their derivatives, such as lauric acid (C12), palmitic acid (C16), stearic acid (C18) and docosanoic acid (C22) have been shown to support the delivery of therapeutic oligonucleotides to non-liver tissues.
[Ref.: Annabelle Biscans, Andrew Coles, Reka Haraszti, Dimas Echeverria, Matthew Hassler, Maire Osborn, Anastasia Khvorova, Diverse lipid conjugates for functional extra-hepatic siRNA delivery in vivo, Nucleic Acids Research, Volume 47, Issue 3, 20 February 2019, Pages 1082–1096, https://doi.org/10.1093/nar/gky1239]
Conjugating a hexadecyl lipophilic chain (C16) to the 2’-O position of the ribose sugar backbone of a fully modified siRNA has been shown to confer safe, potent and durable silencing in the central nervous system (CNS), eye and lung.
[Ref.: Brown, Kirk & Nair, Jayaprakash & Janas, Maja & Angleró-Rodríguez, Yesseinia & Peng, Haiyan & Castellanos-Rizaldos, Elena & Brown, Christopher & Foster, Donald & Kurz, Jeffrey & Allen, Jeff & Maganti, Raj & Li, Jing & Matsuda, Shigeo & Chickering, Tyler & Jung, Michelle & Wassarman, Kelly & Rollins, Jeff & Woods, Lauren & Jadhav, Vasant. (2021). Expanding the Reach of RNAi Therapeutics with Next Generation Lipophilic siRNA Conjugates. 10.21203/rs.3.rs-946835/v1.]
Our 2'-O-C16 CE-Phosphoramidites (LK2592, LK2593, LK2594 and LK2595) and CPGs (BG8-1005, BG8-1006, BG8-1007 and BG8-1008) allow you to easily conjugate a 2’-O hexadecyl modification to your oligonucleotides.
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