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The inhibitory effects of 6-amidino-2-naphthyl-4-guanidinobenzoate X dimethanesulfonate (FUT-175) on the human Hageman factor fragment (HFf), factor Xa, thrombin, plasma kallikrein, and plasmin were studied. FUT-175 inhibited plasma kallikrein most (IC50 = 3.0 X 10(-9) M), followed by HFf (IC50 = 3.3 X 10(-7) M). FUT-175 was found to have an anticoagulant effect in the APTT and PT assay systems of human plasma. The concentration of FUT-175 for twofold increase in the clotting time in the APTT assay system was 5 X 10(-7) M.
Hitomi et al. (Tue,) studied this question.