Objective To evaluate the effectiveness and safety of argatroban made in China in treatment of acute cerebral infarction. Methods 106 patients were divided into study group and control group randomly, 53 patients in each group, Patients in the control group were treated by conventional therapy, such as low molecular dextran, nimodipine, citicoline sodium, and asprin. Argatroban was used in the study group in addition to conventional therapy for 7days. The patients in all groups were observed for another 7days after treatment. NIHSS score was used to evaluate the clinical effect. The changes in aspartate aminotransferase(ALT), prothrombin time(PT), activated partial thromboplastin time(aPTT), blood platelet(PLT) count were used to evaluate the safety. Results There was significant decrease of neurologic impairment scores in study group after treatment for 7 days and 14 days compared with before treatment [(9.28±3.25) vs (14.22±4.27); (7.61±2.44) vs (14.22±4.27), P<0.05]. The post-treatment neurologic impairment scores in the study group were low compared with the control group after treatment for 7 days and 14 days [(9.28±3.25) vs(11.86±3.58)]; [(7.61±2.44) vs (9.40±3.45)], P<0.05) . There were no difference in ALT, PT, aPTT, and PLT before and after treatment in both groups. Conlusions Argatroban is effective for the acute cerebral ischemic stroke and has no obvious bleeding tendency and other side effects. Argatroban is worthy of wide use in cerebral ischemic stroke.