The octylglycosides 1-3 having heparan sulfate fragments were designed as inhibitors specific for human heparanase-1. Inhibition experiments for the heparanase revealed the inhibitory effects of 1 and 3 (IC50 = 6 and 1.4 mM, respectively). It was difficult for compound 2 to inhibit the heparanase activity. Furthermore, the inhibitory action of 3 was specific for the heparanase, whereas 1 and 2 also inhibited the hydrolysis activity of exoenzyme beta-glucuronidase from bovine liver.