Objective To study the metabolites of rodanine derivative Lj0104 in rat plasma in particular. Method Verapamil is utilized as the internal standard (IS). Male Sprague-Dawley rats were administered with compound Lj0104 by po. 5. 0 mg/kg and iv. 1.0 mg/kg. Plasma concentration of the parent compound and the metabolites were analyzed using LC-MS/MS. Result Three major metabolites were discovered. Conclusion The major metabolites of Lj0104 are hydroxylation and hydrolysis products. This study provides guidance for further modification of Lj0104.