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SML3285

Apixaban

Name: Apixaban
Brand: SIGMA

≥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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关于此项目

经验公式（希尔记法）:

C₂₅H₂₅N₅O₄

化学文摘社编号:

503612-47-3

分子量:

459.50

UNSPSC Code:

12352107

NACRES:

NA.77

MDL number:

MFCD11977295

Assay:

≥98% (HPLC)

Form:

powder

Quality level:

100

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属性

产品名称

Apixaban, ≥98% (HPLC)

Quality Level

100

assay

≥98% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

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

说明

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.

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存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

0000499685

0000478630

0000438639

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Arterial antithrombotic and bleeding time effects of apixaban, a direct factor Xa inhibitor, in combination with antiplatelet therapy in rabbits.

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

Pharmacokinetics and Biologic Activity of Apixaban in Healthy Dogs.

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

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 blood coagulation factor Xa.

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

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全球贸易项目编号

货号	GTIN
SML3285-50MG	04065267045030
SML3285-10MG	04065267045023