产品说明书

Darexaban

Print
Chemical Structure| 365462-23-3 同义名 : YM150
CAS号 : 365462-23-3
货号 : A1376680
分子式 : C27H30N4O4
纯度 : 97%
分子量 : 474.551
MDL号 : MFCD16620506
存储条件：

粉末 Keep in dark place,Sealed in dry,Room Temperature

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 250 mg/mL(526.81 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Factor Xa (FXa) is a critical enzyme in the coagulation cascade responsible for thrombin generation, the final enzyme that leads to fibrin clot formation[1]. Darexaban (or YM150) is an oral, direct factor Xa inhibitor, with a Ki for factor Xa of 31 nM. T[2].Darexaban doubled the FXa clotting time and prothrombin time at 2.0 and 1.8 µM, respectively. It also strongly inhibited prothrombin activation induced by free Xa, prothrombinase and whole-blood clots[3].In mice, darexaban inhibited FXa activity in plasma with an ED50 value of 24.8 mg/kg.PT and activated partial thromboplastin time (aPTT) prolonged by darexaban were dose-dependently reversed by intravenously-administered rFVIIa, significantly so at 1 mg/kg. In a FeCl3-induced venous thrombosis (VT) mouse model, darexaban (0.3-10 mg/kg) dose-dependently decreased the thrombus protein content, significantly so at doses of 3 mg/kg or higher. In a tail-transection mouse model, darexaban had no significant effect on the amount of blood loss at doses up to 10 mg/kg, while warfarin showed a dose-dependent increase in blood loss, significantly so from 1 mg/kg/day. Darexaban and its metabolite darexaban glucuronide significantly prolonged PT and aPTT in human plasma in vitro, and while rFVIIa concentration-dependently reversed the prolonged PT in this plasma, ACC dose-dependently reversed both PT and aPTT changes prolonged by darexaban[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.11mL

0.42mL

0.21mL

10.54mL

2.11mL

1.05mL

21.07mL

4.21mL

2.11mL
参考文献

[1] Donald J P Pinto,Jennifer X Qiao,et al. The emergence of factor Xa inhibitors for the treatment of cardiovascular diseases: a patent review. Expert Opin Ther Pat. 2012 Jun;22(6):645-61.

[2]Ji-Woong Jeong,et al. In vitro and in vivo activities of LCB01-0371, a new oxazolidinone. Antimicrob Agents Chemother. 2010 Dec;54(12):5359-62.

[3] Apostolakis S, Lip GY, Lane DA,Shantsila E. The quest for new anticoagulants: from clinical development to clinical practice. Cardiovasc Ther 2011;29:e12-22.

[4]Seiji Kaku, Mami Suzuki,et al. Darexaban: anticoagulant effects in mice and human plasma in vitro, antithrombotic effects in thrombosis and bleeding models in mice and effects of anti-inhibitor coagulant complex and recombinant factor VIIa. Thromb Res. 2013 May;131(5):450-6.