GalNac Delivery System Lipids

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tri-GalNAc-COOH

Catalog: BL-M001373

CAS: 1953146-81-0
GalNac-L96 free base

Catalog: BL-M001374

CAS: 1159408-61-3
GalNAc

Catalog: BL-M001375

CAS: 1159408-72-6
Triantennary GalNAc Ligand

Catalog: BL-M001376

CAS: 1159408-63-5
Tri-GalNAc(OAc)3 TFA

Catalog: BL-M001377

CAS: 1159408-65-7

GalNAc are surface-modified sugar molecules commonly used in stem cell-targeted delivery systems of drugs and biomolecules, typically using lipid nanoparticles and liposomes as carriers for transport. Therefore, such modified GalNAc lipids not only help to form nanoparticles or complexes with therapeutic molecules (e.g. mRNA, peptides, small molecule drugs, ASOs, etc.), but also improve their stability, cellular uptake and targeting specificity. As a liposome expert, BOC Science has the ability to manufacture and supply high-volume and GMP-grade GalNac delivery system liposomes, thus providing high-quality liposome products and related customized services to customers in need.

What are GalNac Delivery System Lipids?

What is GalNac?

N-Acetylgalactosamine (GalNAc) is an aminosugar derivative of galactose, whose general function in living organisms is to form the terminal carbohydrate of the blood antigen type A. GalNAc is usually the first monosaccharide to be O-glycosylated in a specific form of the protein linking serine or threonine. Moreover, GalNAc is important in the exchange of information between cells, especially in sensory neural structures. Most importantly, GalNAc binds specifically to the desialylate glycoprotein receptor on hepatocytes. The desialylate glycoprotein receptor (ASGPR) is a heterologous oligo lectin receptor responsible for mediating endocytosis. It is found only on the surface of the plasma membrane of hepatocytes and specifically binds glycoproteins with non-reducing terminal D-galactose (Gal) or N-acetylgalactosamine (GalNAc) residues.The affinity of ASGPR for GalNAc is approximately 50-fold higher than that for Gal. Therefore, ASGPR is considered a particularly attractive target for drug delivery studies.

Figure 1. The chemical structure of GalNac.

What is GalNac Delivery System?

GalNAc delivery systems, a method commonly used in the field of drug delivery to target liver tissue or hepatocytes, have been instrumental in the development of various therapies, particularly in gene therapy for the delivery of nucleic acid drugs. In particular, combinations of lipids and GalNAc ligands can selectively target GalNAc receptor-rich hepatocytes. Once the GalNAc-lipid-drug complex reaches the liver, it can bind to the receptor on the surface of the hepatocyte, promoting cellular uptake and delivery of the therapeutic substance into the cell. Several experiments have shown that the use of a lipid-based GalNAc delivery system will improve the efficacy of therapy by facilitating stability and minimizing off-target effects.

Figure 2. Schematic representation of the kinetics of the uptake process of GalNAc-modified liposomes at the liver through different signaling pathways. (Y, k, Sato.; et al, 2020)

The Structure of GalNac Lipid

GalNAc ligands for liposome modification contain three basic units, a hydrophilic target group, a lipophilic anchor, and an intermediate linker unit. The structure of the target group, the sugar substituent, the ligand density, the size of the ligand-modified particles, and the structure of the junction all affect the affinity of liposomes for ASGPR. Among them, the structure of the junction significantly affects the affinity for this specific targeting. To choose the right GalNAc lipids for your research needs, at BOC Sciences you have access to expert consulting and customization services.

Figure 3. Structures of CHS-6-GalNAc, CHS-1-Gal, CHS-6-Gal, and CHS-PEG2-6-GalNAc.( H, Nie.; et al, 2022)

Applications of GalNac Delivery System Lipids

Developing Nucleic Acid-Based Drug Therapies

Currently, one of the hottest applications of the GalNAc delivery system is the delivery of various nucleic acid drugs, especially based on siRNAs, ASOs and mRNAs, to the liver for gene therapy. These therapies can be used to target specific genes involved in inherited diseases or metabolic disorders that primarily affect the liver.The GalNAc system delivers lipids that enhance the delivery of therapeutic nucleic acids to the hepatocyte to promote gene silencing or modulation.

Providing New Ideas for Liver Disease Research

GalNAc System Delivery Lipids have a wide range of promising applications in liver disease research such as liver cancer and hepatitis. This has led to more targeted treatments with greater safety and efficacy than some conventional therapies.

Development of Hepatocyte Contrast Agents

In addition to delivering drug molecules, GalNAc delivery system lipids can also be used for tracing by delivering a variety of fluorescent molecules and contrast agents. This has important implications for biological research and the development of hepatocyte contrast agents.

Benifits of BOC Sciences' GalNac Delivery System Lipids

BOC Sciences manufactures and supplies a range of GalNac delivery system lipids products, both GMP and non-GMP grade, that are of high quality.

BOC Sciences implements stringent quality control and optimizes efficient isolation and purification strategies to ensure that you receive high purity GalNac delivery system lipids.

BOC Sciences has a team of experts with master's degrees or higher, and more GalNac delivery system lipids are in development.

With high-end production facilities, optimized production processes and high production efficiency, BOC Sciences is committed to providing you with larger quantities of products and shorter lead times for customized services.

For more custom services about our GalNac delivery system lipids, please feel free to contact us.

References

Y, k, Sato.; et al. Different Kinetics For The Hepatic Uptake Of Lipid Nanoparticles Between The Apolipoprotein E/Low Density Lipoprotein Receptor And The N-Acetyl-D-Galactosamine/Asialoglycoprotein Receptor Pathway. Journal of Controlled Release. 2020, 332: 217-226.
H, Nie.; et al. Effect Of Hydrophile–Lipophile Balance Of The Linker In Gal/Galnac Ligands On High-Affinity Binding Of Galactosylated Liposomes By The Asialoglycoprotein Receptor. International Journal of Pharmaceutics. 2022, 624: 121967.

GalNac Delivery System Lipids

tri-GalNAc-COOH

GalNac-L96 free base

GalNAc

Triantennary GalNAc Ligand