N-(alpha-L-Arabinofuranos-1-yl)-L-cysteine was stereoselectively prepared from L-arabinose and l-cysteine. Its in vivo detoxification action was evaluated on lead loaded mice at the doses of 0.1, 0.2, and 0.4 mmol/kg. The results show that lead accumulation in the livers, kidneys, brains, and femurs of the treated mice could be efficiently decreased by N-(alpha-L-arabinofuranos-1-yl)-L-cysteine, even at the dose of 0.1 mmol/kg. Compared with the lead detoxification efficacy, 0.4 mmol/kg of N-(alpha-L-arabinofuranos-1-yl)-L-cysteine did not affect the essential metals in the treated mice, such as Fe, Cu, Zn, and Ca. In the apparent permeability coefficient test, the values of P(app)(A-->B), P(app)(B-->A), and P(app)(A-->B)/P(app)(B-->A) indicated that N-(alpha-L-arabinofuranos-1-yl)-L-cysteine was transported actively across the Caco-2 cell monolayer. Silico molecular modeling results predicted that N-(alpha-L-arabinofuranos-1-yl)-L-cysteine had no hepatotoxicity.