YM-60828 (methanesulfonate)

YM-60828 methanesulfonate is an orally active, selective and competitive factor Xa inhibitor with a K_i of 1.3 nM and an IC50 of 2.3 nM. YM-60828 methanesulfonate inhibits thrombus formation and platelet aggregation. YM-60828 methanesulfonate can be used for the research of venous thrombosis, arterial thrombosis, and thromboembolic disorders^{[1][2][3][4][5]}. In Vitro:YM-60828 methanesulfonate potently prolongs prothrombin time in pooled mouse plasma, with a CT₂ value of 0.70 μM^[2].
YM-60828 (3 min) methanesulfonate dose-dependently prolongs human plasma factor Xa clotting time, prothrombin time, and activated partial thromboplastin time, with CT₂ values of 0.10 μM, 0.21 μM, and 0.24 μM respectively, and does not affect thrombin time at concentrations up to 100 μM^[5].
YM-60828 methanesulfonate dose-dependently prolongs prothrombin time and activated partial thromboplastin time in plasma from multiple species, with the highest potency in squirrel monkey plasma (CT₂ 0.16 μM for PT, 0.18 μM for APTT) and lowest potency in guinea pig plasma (CT₂ 2.79 μM for PT, 1.36 μM for APTT)^[5].
YM-60828 (0.1-100 nM) methanesulfonate dose-dependently inhibits thrombin generation in the prothrombinase complex on washed human platelet surfaces, with an IC₅₀ of 7.7 nM^[5].
YM-60828 methanesulfonate dose-dependently inhibits agonist-induced aggregation of human platelets, with IC₅₀ values ranging from 3.3 μM (TRAP-induced in PRP) to 23.4 μM (Thrombin-induced in washed platelets)^[5]. In Vivo:YM-60828 (i.v.; single dose) methanesulfonate dose-dependently inhibits venous thrombus formation in guinea pigs, with an ID₅₀ of 0.012 mg/kg and significant activity at 0.03 mg/kg^[1].
YM-60828 (i.v.; single dose) methanesulfonate dose-dependently inhibits thrombus formation in a guinea pig arterio-venous shunt model, with an ID₅₀ of 0.0094 mg/kg and significant activity at 0.01 mg/kg^[1].
YM-60828 (i.v.; single dose) methanesulfonate dose-dependently inhibits carotid artery thrombus formation in guinea pigs, with an ID₅₀ of 0.14 mg/kg and significant activity at 0.3 mg/kg^[1].
YM-60828 (100 mg/kg; p.o.; single dose) methanesulfonate exhibits anticoagulant activity in ICR mice^[2].
YM-60828 (0.1-1 mg/kg bolus + 0.3-3 mg/kg/h infusion; i.v.; 60 min) methanesulfonate dose-dependently improves carotid artery patency after moPA-induced thrombolysis in rats with electrically-induced arterial thrombosis^[3].
YM-60828 (10-100 mg/kg; p.o.; single dose; 60 min pre-stimulation) methanesulfonate improves carotid artery patency in a rat arterial thrombosis model^[4].
YM-60828 (0.3 (i.v.) and 3 mg/kg (p.o.); single dose) methanesulfonate exhibits anticoagulant activity in squirrel monkeys^[5].