A peracetylated β-D-N-acetylgalactosamine (GalNAcβ) ligand equipped with a terminal carboxylic acid through a short butyl spacer, with the sugar hydroxyl groups protected as acetate esters. The peracetate groups increase lipophilicity to facilitate cell membrane permeability. The carboxylic acid can be activated to NHS, sulfo-NHS, or pentafluorophenyl (PFP) esters and reacted with amine-functionalized platforms or lysine residues on proteins and peptides to form stable amide bonds. This compound enables the construction of hepatocyte-targeted therapeutics and research tools that exploit the asialoglycoprotein receptor (ASGPR), which is highly expressed on liver hepatocytes and binds GalNAc-containing ligands with high affinity.