DX-9065a, a new synthetic, potent anticoagulant and selective inhibitor for factor Xa.
作者： Tsuyoshi Hara , Asako Yokoyama , Hiroaki Ishihara , Yukio Yokoyama , Takayasu Nagahara
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摘要: DX-9065a is an orally active newly synthesized and specific inhibitor for factor Xa. We have examined the property of in vitro ex vivo. prolonged human plasma recalcification time, APTT PT. Its doubling concentrations clotting times each coagulation assay were 0.49, 0.97 0.52 microM, respectively. Kinetic study revealed that inhibited competitively Xa (Ki value: 41 nM). Ki values (microM) other serine proteases as follows; thrombin > 2000, trypsin 0.62, chymotrypsin plasmin 23, t-PA 21, kallikrein 2.3 tissue 1000. up to 100 microM had no effects on platelet aggregation. After intravenous or oral administration, significantly PT with a dose dependent manner. These well correlated anti-Xa activity plasma. results suggest may become anticoagulant by means inhibition
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