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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产品名称 | Factor Xa ↓ ↑ | 其他靶点 | 纯度 | ||||||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Rivaroxaban |
++
Factor Xa, IC50: 0.7 nM |
98% | |||||||||||||||||
Apixaban |
++++
Factor Xa (rabbit), Ki: 0.17 nM Factor Xa (human), Ki: 0.08 nM |
98% | |||||||||||||||||
Edoxaban tosylate monohydrate |
+++
Factor Xa, Ki: 0.561 nM |
98+% | |||||||||||||||||
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。 |
靶点 |
|
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]. |
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 |
|
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 | - | |
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 |
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 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Sealed in dry,Store in freezer, under -20°C |
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 |