Apixaban

製品コードS1593 バッチS159303

印刷

化学情報

Chemical Structure Synonyms BMS 562247-01 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H25N5O4
分子量 459.5 CAS No. 503612-47-3
Solubility (25°C)* 体外 DMSO 18 mg/mL (39.17 mM)
Water Insoluble
Ethanol Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
30%PEG400 0.5%Tween80 5%Propylene glycol
30.0mg/ml Taking the 1 mL working solution as an example, add 300 μL of 100 mg/ml clarified PEG400 stock solution to 5 μL of Tween80, mix evenly to clarify it; add 50 μL Propylene glycol to the above system, mix evenly to clarify it; then continue to add 645 μL ddH2O to adjust the volume. to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Apixaban is a highly selective, reversible inhibitor of Factor Xa with Ki of 0.08 nM and 0.17 nM in human and rabbit, respectively.
in vitro

Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor Xa with Ki of 0.08 nM and 0.17 nM for Human Factor Xa and Rabbit Factor Xa, respectively. [1]

In vitro, Apixaban prolongs the clotting times of normal human plasma with the concentrations (EC2x) of 3.6 μM, 0.37 μM, 7.4 μM, and 0.4 μM, which are required respectively to double the prothrombin time (PT), modified prothrombin time (mPT), activated partial thromboplastin time (APTT) and HepTest. Besides, Apixaban shows the highest potency in human and rabbit plasma, but less potency in rat and dog plasma in both the PT and APTT assays. [2]
in vivo

In the dog, Apixaban shows the excellent pharmacokinetics with very low clearance (Cl: 0.02 L kg-1 h-1), and low volume of distribution (Vdss: 0.2 L kg-1). Besides, Apixaban also exhibits a moderate half-life (T1/2: 5.8 hours) and good oral bioavailability (F: 58%). [1]

In the arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models, Apixaban produces dose-dependent antithrombotic effects with EC50 of 270 nM, 110 nM and 70 nM, respectively. [2]

Apixaban significantly inhibits factor Xa activity with IC50 of 0.22 μM in rabbit ex vivo. [3]

In chimpanzee, Apixaban also shows small volume of distribution (Vdss: 0.17 L kg-1), low systemic clearance (Cl: 0.018 L kg-1 h-1), and good oral bioavailability (F: 59%). [4]
特徴 A highly selective, reversible, and direct factor Xa inhibitor.

プロトコル(参考用のみ)

キナーゼアッセイ Enzyme Affinity Assays.
All enzyme Ki values are obtained from purified human enzymes. All fXa assays are run in microtiter plates using a total volume of 250 μL in 0.1 M sodium phosphate buffer containing 0.2 M NaCl and 0.5% polyethylene glycol 6000 at pH 7.0. Apixaban are run at 10 μM, 3.16 μM, 1.0 μM, 0.316 μM, 0.1 μM, 0.0316 μM, 0.01 μM, and 0.00316 μM. Plates are read for 30 minutes at 405 nm. Rates are determined in the presence of the controls (no inhibitor) and for the inhibitors. Apixaban are tested in duplicate studies and are compared with the same internal standards. The intraassay and interassay variabilities are 5% and 20%, respectively. All of the enzyme assays are conducted in pH 7.4 buffer at room temperature. All enzymes are purified from human tissues and are obtained from commercially available sources. Individual enzyme and substrate Km are determined in separate experiments and are close to values established in the literature. Steady-state inhibition of enzyme activity is determined by incubating a range of inhibitor concentrations (1 nM to 50 μM, in duplicate) with fixed enzyme (0.1 nM−100 nM) and peptide substrate (200 μM−1000 μM) concentration for up to 30 minutes. The Ki is calculated, assuming competitive inhibition and one-site binding, either from the IC50 or from the extent of inhibition at each inhibitor concentration.
細胞アッセイ 細胞株 Cell-free assays
濃度 0.08 nM
反応時間
実験の流れ
動物実験 動物モデル Arteriovenous-shunt thrombosis (AVST), venous thrombosis (VT) and electrically mediated carotid arterial thrombosis (ECAT) rabbit models.
投薬量 ≤3 mg/kg/h
投与方法 Administered via i.v.

カスタマーフィードバック

Data from [Data independently produced by , , Sci Rep, 2016, 6:29387]

Data from [Data independently produced by , , Neuroscience, 2018, 371:445-454]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Rivaroxaban attenuates neutrophil maturation in the bone marrow niche [ Basic Res Cardiol, 2023, 118(1):31] PubMed: 37580509
OKL-1111, A modified cyclodextrin as a potential universal reversal agent for anticoagulants [ Thromb Res, 2023, 227:17-24] PubMed: 37207560
Factor VII, EPCR, aPC Modulators: novel treatment for neuroinflammation [ J Neuroinflammation, 2022, 19(1):138] PubMed: 35690769
Evaluation of Xa inhibitors as potential inhibitors of the SARS-CoV-2 Mpro protease [ PLoS One, 2022, 17(1):e0262482] PubMed: 35015795
In vitro reversal of direct factor Xa inhibitors: Direct comparison of andexanet alfa and prothrombin complex concentrates Cofact and Beriplex/Kcentra [ Res Pract Thromb Haemost, 2022, 6(5):e12775] PubMed: 35928523
Markers for neural degeneration and regeneration: novel highly sensitive methods for the measurement of thrombin and activated protein C in human cerebrospinal fluid [ Neural Regen Res, 2021, 16(10):2086-2092] PubMed: 33642398
An engineered factor Va prevents bleeding induced by direct-acting oral anticoagulants by different mechanisms [ Blood Adv, 2020, 4(15):3716-3727] PubMed: 32777068
A Novel Highly Sensitive Method for Measuring Inflammatory Neural-Derived APC Activity in Glial Cell Lines, Mouse Brain and Human CSF [ Int J Mol Sci, 2020, 31;21(7):2422] PubMed: 32244492
The Anticoagulant Nafamostat Potently Inhibits SARS-CoV-2 S Protein-Mediated Fusion in a Cell Fusion Assay System and Viral Infection In Vitro in a Cell-Type-Dependent Manner [ Viruses, 2020, 10;12(6):E629] PubMed: 32532094
D-Dimer and Fibrin Degradation Products Impair Platelet Signaling: Plasma D-Dimer Is a Predictor and Mediator of Platelet Dysfunction During Trauma [ J Appl Lab Med, 2020, jfaa047] PubMed: 32674119

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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