Darexaban

Research use only, not for human use.

A potent, selective and orally available factor Xa (FXa) inhibitor with IC50 of 54.6 nM.

A potent, selective and orally available factor Xa (FXa) inhibitor with IC50 of 54.6 nM; displays high selectivities over other related serine proteases, such as trypsin, thrombin and kallikrein (IC50>10 uM); demonstrates potent anticoagulant activities both in vitro and in vivo, shows potential for prevention and treatment of thromboembolic diseases.Thrombosis Phase 2 Discontinued.

Darexaban is an oral direct factor Xa (FXa) inhibitor that is rapidly and extensively metabolized into its glucuronide conjugate (YM-222714) post-administration. Darexaban competitively and selectively inhibits human FXa, and also inhibits the prothrombin activation induced by prothrombinase complex or whole blood clot with similar potency to free FXa.

In mice, Darexaban inhibits FXa activity in plasma with an ED50 value of 24.8 mg/kg. Darexaban prolonges prothrombin time (PT) at 3 mg/kg. In a pulmonary thromboembolism (PE) mouse model, Darexaban dose-dependently reduces the mortality rate, significantly so at 10 mg/kg.In a FeCl3-induced venous thrombosis (VT) mouse model, Darexaban (0.3-10 mg/kg) dose-dependently decreases the thrombus protein content, significantly so at doses of 3 mg/kg or higher.

YM150 | YM-150 | YM 150

Metabolic Enzyme/Protease

Factor Xa

Factor Xa

Cardiovascular Disease

Thrombosis

365462-23-3

474.561

C27H30N4O4

>98% (HPLC)

In Vitro:?DMSO : 250 mg/mL (526.81 mM)

O=C(NC1=C(NC(C2=CC=C(OC)C=C2)=O)C=CC=C1O)C3=CC=C(N4CCN(C)CCC4)C=C3

N-[2-hydroxy-6-(4-methoxybenzamido)phenyl]-4- (4-methyl-1,4-diazepan-1-yl)benzamide

(-20℃)

With Ice Pack

≥ 2 years