In order to reveal the antithrombotic mechanism of propylene glycol mannite sulfate (PGMS) on gene level and explore the correlation between PGMS and fibrinolytic system, the urokinase-type plasminogen activator (uPA) mRNA expression and uPA activity were detected in vitro and in vivo with semi-quantitative reverse transcription (RT)-PCR and chromogenic method. The results showed that PGMS was able to increase uPA activity in dosage-dependent manner in rat plasma, which resulted in the increase of rat fibrinolytic activity. The change of rat uPA mRNA expression with PGMS was similar to that of uPA activity. The results of experiments with cultured cells were similar to those results of experiments in vivo. The uPA mRNA expression and activities of cultured cells showed increases with PGMS in a concentration-dependent manner. All of these results indicated that PGMS may induce the expression of uPA mRNA. The increase of uPA mRNA expression may therefore reflect, in part, an increase in the stability of uPA mRNA and/or processing of nuclear uPA transcription, which, in turn, may increase the uPA activity in rat plasma and trigger the fibrinolytic system.