产品说明书

Apixaban

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Chemical Structure| 503612-47-3 同义名 : BMS-562247-01
CAS号 : 503612-47-3
货号 : A334174
分子式 : C25H25N5O4
纯度 : 98%
分子量 : 459.497
MDL号 : MFCD11977295
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

生物活性
靶点

  • Factor Xa

    Factor Xa (human), Ki:0.08 nM

    Factor Xa (rabbit), Ki:0.17 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].
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 -
实验方案
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
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