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经验公式(希尔记法):
C25H25N5O4
化学文摘社编号:
分子量:
459.50
UNSPSC Code:
12352107
NACRES:
NA.77
MDL number:
产品名称
Apixaban, ≥98% (HPLC)
SMILES string
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
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Quality Level
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Biochem/physiol Actions
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).
Orally active, active site-targeting, highly potent and selective factor Xa (FXa) inhibitor with antithrombotic efficacy in vitro and in vivo.
存储类别
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
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
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
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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