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Merck
CN

SML3285

Sigma-Aldrich

Apixaban

≥98% (HPLC), powder, Factor Xa (FXa) inhibitor

别名:

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, 4,5,6,7-Tetrahydro-1-(4-methoxyphenyl)-7-oxo-6-[4-(2-oxo-1-piperidinyl)phenyl]-1H-pyrazolo[3,4-c]pyridine-3-carboxamide, BMS 562247, BMS-562247, BMS562247

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About This Item

经验公式(希尔记法):
C25H25N5O4
分子量:
459.50
MDL编号:
UNSPSC代码:
12352107
NACRES:
NA.77

产品名称

Apixaban, ≥98% (HPLC)

质量水平

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

N5(CCCCC5=O)c1ccc(cc1)N2CCc3c([n](nc3C(=O)N)c4ccc(cc4)OC)C2=O

InChI

1S/C25H25N5O4/c1-34-19-11-9-18(10-12-19)30-23-20(22(27-30)24(26)32)13-15-29(25(23)33)17-7-5-16(6-8-17)28-14-3-2-4-21(28)31/h5-12H,2-4,13-15H2,1H3,(H2,26,32)

InChI key

QNZCBYKSOIHPEH-UHFFFAOYSA-N

生化/生理作用

Apixaban is an orally active, active site-targeting, highly potent and selective factor Xa (FXa) inhibitor (human/rabbit Ki = 0.08/0.17 nM; trypsin Ki >3 μM) with good anticoagulant activity in vitro (EC2x = 3.8 μM by prothrombin time (PT) assay, 5.1 μM by activated partial thromboplastin time (aPTT) assay) and antithrombotic efficacy in vivo (IC50 = 329 nM i.v. by rabbit arteriovenous shunt model).

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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分析证书(COA)

Lot/Batch Number

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P L A Giesen et al.
Thrombosis journal, 19(1), 60-60 (2021-08-30)
Thrombin generation (TG) assessed by Calibrated Automated Thrombogram (CAT-I) reflects the overall capacity of plasma to generate thrombin, thus evaluating the balance between the anti- and procoagulant processes. However, with this method the calibrator curve is usually not measured until
P C Wong et al.
Journal of thrombosis and haemostasis : JTH, 6(5), 820-829 (2008-03-05)
Apixaban is an oral, direct and highly selective factor Xa (FXa) inhibitor in late-stage clinical development for the prevention and treatment of thromboembolic diseases. We evaluated the in vitro properties of apixaban and its in vivo activities in rabbit models
Noelle D Herrera et al.
Frontiers in veterinary science, 8, 702821-702821 (2021-07-23)
Thrombosis is common in critically ill dogs and causes considerable morbidity and mortality. The direct factor Xa inhibitor apixaban is safe, efficacious, and convenient in humans. This study aimed to determine the pharmacokinetics (PK), bioactivity, protein binding, and bioavailability of
Donald J P Pinto et al.
Journal of medicinal chemistry, 50(22), 5339-5356 (2007-10-05)
Efforts to identify a suitable follow-on compound to razaxaban (compound 4) focused on modification of the carboxamido linker to eliminate potential in vivo hydrolysis to a primary aniline. Cyclization of the carboxamido linker to the novel bicyclic tetrahydropyrazolopyridinone scaffold retained
P C Wong et al.
Journal of thrombosis and haemostasis : JTH, 6(10), 1736-1741 (2008-07-24)
Optimal treatment of arterial thrombosis may include a combination of antiplatelet and anticoagulant drugs. We evaluated apixaban, a direct and highly selective factor Xa inhibitor, in combination with clinically relevant doses of aspirin and/or clopidogrel for prevention of arterial thrombosis

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