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Darexaban {[allProObj[0].p_purity_real_show]}

货号:A1376680 同义名: YM150 Ambeed 开学季,买赠积分,赢豪礼

Darexaban is a potent and orally effective factor Xa inhibitor with IC50 value of 54.6nM.

Darexaban 化学结构 CAS号:365462-23-3
Darexaban 化学结构
CAS号:365462-23-3
Darexaban 3D分子结构
CAS号:365462-23-3
Darexaban 化学结构 CAS号:365462-23-3
Darexaban 3D分子结构 CAS号:365462-23-3
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Darexaban 纯度/质量文件 产品仅供科研

货号:A1376680 标准纯度: {[allProObj[0].p_purity_real_show]}
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产品名称 Factor Xa 其他靶点 纯度
Rivaroxaban ++

Factor Xa, IC50: 0.7 nM

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Apixaban ++++

Factor Xa (rabbit), Ki: 0.17 nM

Factor Xa (human), Ki: 0.08 nM

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Edoxaban tosylate monohydrate +++

Factor Xa, Ki: 0.561 nM

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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。

Darexaban 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].

Darexaban 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.

Darexaban 实验方案

计算器
存储液制备 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

Darexaban 技术信息

CAS号365462-23-3
分子式C27H30N4O4
分子量 474.551
别名 YM150
运输蓝冰
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

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