Azido-PEG4-alpha-D-glucose is a PEG linker containing azide group and D-glucose moieties. The azide group enables copper-catalyzed Click Chemistry reactions with alkynes, DBCO and BCN. The hydrophilic PEG spacer increases solubility in aqueous media. D-glucose increases solubility in aqueous media and increases the selectivity of the PEGylation reaction.