Inhibitory effect of a new synthetic protease inhibitor (FUT-175) on the coagulation system.
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
Y
Y
Ikari
N
N
Fujii
S
S
D000925:Anticoagulants; D001550:Benzamidines; D001777:Blood Coagulation / Q000187:drug effects*; D005170:Factor X / Q000037:antagonists & inhibitors; D005174:Factor XII / Q000037:antagonists & inhibitors; D015956:Factor XIIa; D015951:Factor Xa; D005341:Fibrinolysin / Q000037:antagonists & inhibitors; D006146:Guanidines / Q000494:pharmacology*; D006801:Humans; D066298:In Vitro Techniques; D007610:Kallikreins / Q000037:antagonists & inhibitors; D010446:Peptide Fragments / Q000037:antagonists & inhibitors; D011480:Protease Inhibitors / Q000494:pharmacology; D013917:Thrombin / Q000037:antagonists & inhibitors
D000925:Anticoagulants; D001550:Benzamidines; D006146:Guanidines; D010446:Peptide Fragments; D011480:Protease Inhibitors; D005170:Factor X; D005174:Factor XII; D007610:Kallikreins; D015956:Factor XIIa; D013917:Thrombin; D015951:Factor Xa; D005341:Fibrinolysin; C032855:nafamostat