It is well accepted that organoselenium compounds are powerful antioxidants that have potential therapeutic benefits. Unfortunately, the therapeutic value of many of these selenium-containing entities is often hampered by low solubility in aqueous solutions, which prevents them from reaching therapeutically relevant doses in plasma. We approached this problem by constructing selenosugars with infinite water solubilities. Work over many years led to the discovery of 1,4-anhydro-4-seleno-d-tallitol (SeTal), which has been shown to accelerate skin-tissue repair, heal wounds in (db/db and wt) rodent and porcine models, and prevent high-glucose-induced endothelial dysfunction in mouse aorta. This lead compound is currently being developed as a topical medicament for a variety of skin-repair scenarios. This article discusses the chemistry that led to the development of our selenium-containing carbohydrates, and showcases the remarkable therapeutic properties of SeTal.