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阿哌沙班 /Apixaban {[allProObj[0].p_purity_real_show]}

货号:A334174 同义名: BMS-562247-01 Ambeed 开学季,买赠积分,赢豪礼

Apixaban is a direct factor Xa inhibitor with an IC50 of 0.08 nM and 0.17 nM in human and rabbit, respectively.

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Apixaban 化学结构 CAS号:503612-47-3
Apixaban 化学结构
CAS号:503612-47-3
Apixaban 3D分子结构
CAS号:503612-47-3
Apixaban 化学结构 CAS号:503612-47-3
Apixaban 3D分子结构 CAS号:503612-47-3
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Apixaban 纯度/质量文件 产品仅供科研

货号:A334174 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。

Apixaban 生物活性

靶点
  • Factor Xa

    Factor Xa (rabbit), Ki:0.17 nM

    Factor Xa (human), Ki:0.08 nM

描述 Apixaban (BMS-562247-01) is a potent, selective, reversible, and orally active inhibitor of Factor Xa, displaying inhibition constants of 0.08 nM in humans and 0.17 nM in rabbits. It is currently being developed for the prevention and treatment of various thromboembolic conditions[1]. Apixaban is applied for the prevention and treatment of various thromboembolic diseases[2].
体内研究

Pharmacokinetically, Apixaban demonstrates low clearance (Cl: 0.02 L/kg/h) and volume of distribution (Vdss: 0.2 L/kg) in dogs, along with a moderate half-life (T1/2: 5.8 hours) and good oral bioavailability (F: 58%). This profile underscores its potential for consistent and predictable dosing in clinical settings[1].

In various rabbit models of thrombosis—arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT), and electrically mediated carotid arterial thrombosis (ECAT)—Apixaban demonstrates dose-dependent antithrombotic effects. The effective concentrations (EC50) required for these effects are 270 nM, 110 nM, and 70 nM, respectively, highlighting its efficacy in inhibiting thrombosis across different vascular contexts[2].

Additionally, Apixaban effectively inhibits factor Xa activity with an IC50 of 0.22 μM in rabbit ex vivo, confirming its potent anti-factor Xa activity beyond human models[3].

In chimpanzees, Apixaban also exhibits a favorable pharmacokinetic profile with a small volume of distribution (Vdss: 0.17 L/kg), low systemic clearance (Cl: 0.018 L/kg/h), and good oral bioavailability (F: 59%)[4].

体外研究

In laboratory tests, Apixaban notably prolongs clotting times in normal human plasma; concentrations (EC2x) of 3.6 μM, 0.37 μM, 7.4 μM, and 0.4 μM are required to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT), and HepTest, respectively. It shows the greatest efficacy in human and rabbit plasma, while exhibiting lesser potency in rat and dog plasma in both PT and APTT assays[2].

Apixaban 动物研究

Dose Rat: 0.1 mg/kg - 3 mg/kg[3] (i.v.) Rabbit: 0.015 mg/kg - 0.5 mg/kg[4] (i.v.) Horse: 0.15 mg/kg - 0.2 mg/kg[5] (p.o./i.v.)
Administration i.v., p.o.
Pharmacokinetics
Animal Rats[3] Dogs[3]
Dose 0.5 mg/kg (i.v.)
2 mg/kg (p.o.)
0.2 mg/kg (i.v.)
0.5 mg/kg (p.o.)
Administration i.v.
p.o.
i.v.
p.o.
F 34% (p.o.) 88% (p.o.)
AUC0→24h 2.0 μg·h/ml (i.v.)
2.7 μg·h/ml (p.o.)
3.9 μg·h/ml (i.v.)
8.0 μg·h/ml (p.o.)
T1/2 1.9 h (i.v.)
3.2 h (p.o.)
5 h (i.v.)
5.8 h (p.o.)
Tmax 0.5 h (p.o.) 1.0 h (p.o.)
CL/F (CLTp) 0.87 ml/min/kg (i.v.)
CL/F 4.3 ml/min/kg (i.v.)
Protein binding (free drug %) 95.2 - 96.4% (i.v.) 91.0 - 93.7% (i.v.)
MRT 1.2 h (i.v.)
3.2 h (p.o.)
5.8 h (i.v.)
8.0 h (p.o.)
Vd 0.31 L/kg (i.v.) 0.30 L/kg (i.v.)
Cmax 1.1 μg/ml (p.o.) 1.1 μg/ml (p.o.)

Apixaban 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT02492828 - Completed - -
NCT01780987 Deep Vein Thrombosis ... 展开 >> Pulmonary Embolism 收起 << Phase 3 Completed - Japan ... 展开 >> Aichi Medical University Hospital Nagakute, Aichi, Japan, 480-1195 Toho University Sakura Medical Center Sakura, Chiba, Japan, 285-8741 Kokura Memorial Hospital Kitakyusyu, Fukuoka, Japan, 802-8555 Hiroshima General Hospital Hatsukaichi, Hiroshima, Japan, 738-8503 Teine Keijinkai Hospital Sapporo, Hokkaido, Japan, 006-8555 Kanazawa Medical University Hospital Kahoku-gun, Ishikawa, Japan, 920-0293 Yokohama Minami Kyousai Hospital Yokohama, Kanagawa, Japan, 236-0037 National Hospital Organization Yokohama Medical Center Yokohama, Kanagawa, Japan, 245-8575 Mie University Hospital Tsu, MIE, Japan, 514-8507 National Hospital Organization Okayama Medical Center Okayama City, Okayama, Japan, 701-1192 Kinki University Hospital Osakasayama, Osaka, Japan, 589-8511 National Cerebral and Cardiovascular Center Hospital Suita-shi, Osaka, Japan, 565-8565 St. Luke's International Hospital Chuo-ku, Tokyo, Japan, 104-8560 Nihon University Itabashi Hospital Itabashi-ku, Tokyo, Japan, 173-8610 National Hospital Organization Tokyo Medical Center Meguro-ku, Tokyo, Japan, 152-8902 Japanese Red Cross Musashino Hospital Musashino, Tokyo, Japan, 180-8610 Tokyo Medical University Hospital Shinjuku-ku, Tokyo, Japan, 160-0023 Fukushima Medical University Hospital Fukushima, Japan, 960-1295 Kumamoto University Hospital Kumamoto, Japan, 860-8556 Saiseikai Kumamoto Hospital Kumamoto, Japan, 861-4193 收起 <<
NCT02640222 - Active, not recruiting December 31, 2019 -

Apixaban 参考文献

[1]Pinto DJ, et al. Discovery of 1-(4-methoxyphenyl)-7-oxo-6-(4-(2-oxopiperidin-1-yl)phenyl)-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine-3-carboxamide (apixaban, BMS-562247), a highly potent, selective, efficacious, and orally bioavailable inhibitor of blo

[2]Wong PC, et al. Apixaban, an oral, direct and highly selective factor Xa inhibitor: in vitro, antithrombotic and antihemostatic studies. J Thromb Haemost. 2008 May;6(5):820-9

[3]Zhang D, et al. Metabolism, pharmacokinetics and pharmacodynamics of the factor Xa inhibitor apixaban in rabbits. J Thromb Thrombolysis. 2010 Jan;29(1):70-80

[4]He K, et al. Preclinical pharmacokinetics and pharmacodynamics of apixaban, a potent and selective factor Xa inhibitor. Eur J Drug Metab Pharmacokinet. 2011 Sep;36(3):129-39

Apixaban 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.18mL

0.44mL

0.22mL

10.88mL

2.18mL

1.09mL

21.76mL

4.35mL

2.18mL

Apixaban 技术信息

CAS号503612-47-3
分子式C25H25N5O4
分子量 459.497
别名 BMS-562247-01
运输蓝冰
存储条件

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度

DMSO: 50 mg/mL(108.81 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

IP 2% DMSO+water 0.4 mg/mL clear

PO 0.5% CMC-Na 45 mg/mL suspension

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