Apixaban

別名：BMS 562247-01

製品コード：S1593 純度：99.98%

Apixaban is a highly selective, reversible inhibitor of Factor Xa with K_i of 0.08 nM and 0.17 nM in human and rabbit, respectively.

CAS No. 503612-47-3

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 63000	国内在庫あり
10mg	JPY 48000	国内在庫あり
50mg	JPY 145500	国内在庫あり
1g	JPY 598500	国内在庫なし(納期7~10日)

代表番号: 045-509-1970\|電子メール：[email protected] よく尋ねられる質問

文献中Selleckの製品使用例（28）

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製品安全説明書

現在のバッチを見る：純度： 99.98%

99.98

Apixaban関連製品

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シグナル伝達経路

Factor Xaシグナル伝達経路

Factor Xa阻害剤の選択性比較

Cell Data

Cell Lines	Assay Type	Incubation Time	活性情報	PMID
Caco-2	Function assay	48 hrs	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging, IC50=5.91μM	ChEMBL
Caco-2	Toxicity assay	48 hrs	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay, CC50=18.07μM	ChEMBL
A673	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells	29435139
BT-37	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells	29435139
SJ-GBM2	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for SJ-GBM2 cells	29435139
Rh41	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh41 cells	29435139
RD	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for RD cells	29435139
Rh30	qHTS assay		qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Confirmatory screen for Rh30 cells	29435139
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

生物活性

製品説明

Apixaban is a highly selective, reversible inhibitor of Factor Xa with K_i of 0.08 nM and 0.17 nM in human and rabbit, respectively.

特性

A highly selective, reversible, and direct factor Xa inhibitor.

Targets

Factor Xa (human) ^[1] (Cell-free assay)	Factor Xa (rabbit) ^[1] (Cell-free assay)
0.08 nM(Ki)	0.17 nM(Ki)

In Vitro
In vitro	Apixaban exhibits a high degree of potency, selectivity, and efficacy on Factor Xa with K_i 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 (EC_2x) 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]
Kinase Assay	Enzyme Affinity Assays.
Kinase Assay	All enzyme K_i 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.

In Vivo
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 (V_dss: 0.2 L kg^-1). Besides, Apixaban also exhibits a moderate half-life (T_1/2: 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 (V_dss: 0.17 L kg^-1), low systemic clearance (Cl: 0.018 L kg^-1 h^-1), and good oral bioavailability (F: 59%). ^[4]
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.
	投与量	≤3 mg/kg/h
	投与経路	Administered via i.v.

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06388239	Not yet recruiting	Healthy Volunteer	International Bio service	August 26 2024	Phase 1
NCT05869591	Recruiting	Liver Cirrhosis	Centre Hospitalier Universitaire Vaudois	January 18 2024	Phase 2
NCT05683808	Not yet recruiting	Glioblastoma\|Astrocytoma\|Venous Thromboembolism	University of Vermont Medical Center\|Dartmouth-Hitchcock Medical Center\|MaineHealth	January 16 2023	Phase 2

参考
[1] Pinto DJ, et al. J Med Chem. 2007, 50(22), 5339-5356. [2] Wong PC, et al. J Thromb Haemost. 2008, 6(5), 820-829. [3] Zhang D, et al. J Thromb Thrombolysis. 2010, 29(1), 70-80. [4] He K, et al. Eur J Drug Metab Pharmacokinet. 2011, 36(3), 129-139. + 展開

参考

[4] He K, et al. Eur J Drug Metab Pharmacokinet. 2011, 36(3), 129-139.

+ 展開

化学情報

分子量	459.5	化学式	C₂₅H₂₅N₅O₄
CAS No.	503612-47-3	SDF	Download Apixaban SDFをダウンロードする
Smiles	COC1=CC=C(C=C1)N2C3=C(CCN(C3=O)C4=CC=C(C=C4)N5CCCCC5=O)C(=N2)C(=O)N
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 18 mg/mL ( (39.17 mM)；吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Water : Insoluble

Ethanol : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

投与溶液組成計算機(クリア溶液)

ステップ１：実験データを入力してください。（実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

ステップ２：投与溶媒の組成を入力してください。（ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください）

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

計算結果：

投与溶媒濃度： mg/ml;

DMSOストック溶液調製方法： mg 試薬を μL DMSOに溶解する（濃度 mg/mL, 注：濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法：Take μL DMSOストック溶液に μL PEG300，を加え、完全溶解後μL Tween 80，を加えて完全溶解させた後 μL ddH₂O，を加え完全に溶解させます。

投与溶媒調製方法：μL DMSOストック溶液に μL Corn oil，を加え、完全溶解。

注意：１.ストック溶液に沈殿、混濁などがないことをご確認ください；
２.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

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Handling Instructions

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C8=C7/X	C8:	LOG(C8):