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Edoxaban

因子Xa抑制剂，Edoxaban(DU-176)是口服的FXa抑制剂，临床开发用于中风预

目录号: PC15629 纯度: ≥98%

CAS No. :480449-70-5

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PC15629-5mg	5mg	¥735.00	请登录
PC15629-10mg	10mg	¥1215.20	请登录
PC15629-50mg	50mg	¥4596.20	请登录
PC15629-200mg	200mg	¥12083.40	请登录
PC15629-10mM (in 1mL DMSO)	10mM (in 1mL DMSO)	¥4508.00	请登录

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中文名称

Edoxaban

中文别名

伊多塞班;N-(5-氯-2-吡啶基)-N'-[(1S,2R,4S)-4-[(二甲基氨基)甲酰基]-2-[[(4,5,6,7-四氢-5-甲基噻唑并[5,4-c]吡啶-2-基)甲酰]氨基]环己基]乙二酰胺;依杜沙班标准品;依度沙班;依多沙班;依度沙班杂质

英文名称

Edoxaban

英文别名

Edoxaban;N-(5-Chloro-2-pyridinyl)-N'-[(1S,2R,4S)-4-[(dimethylamino)carbonyl]-2-[[(4,5,6,7-tetrahydro-5-methylthiazolo[5,4-c]pyridin-2-yl)carbonyl]amino]cyclohexyl]ethanediamide;DU-176;EthanediaMide,N1-(5-chloro-2-pyridinyl)-N2-[(1S,2R,4S)-4-[(diMethylaMino)carbonyl]-2-[[(4,5,6,7-tetrahydro-5-Methylthiazolo[5,4-c]pyridin-2-yl)carbonyl]aMino]cyclohexyl];Edoxaban iMpurities;Lixiana;SAVAYSA;NDU3J18APO;Edoxaban hydrochloride;C24H30ClN7O4S;N1-(5-chloropyridin-2-yl)-N2-((1S,2R,4S)-4-(dimethylcarbamoyl)-2-(5-methyl-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridine-2-carboxamido)cyclohexyl)oxalamide;Edoxaban [USAN:INN];Edoxaban (USAN/INN);GTPL7575;HGVDHZBSSITLCT-JLJPHGGASA-N;AOB87348;BDBM50328731;PB31142

Cas No.

480449-70-5

分子式

C₂₄H₃₀ClN₇O₄S

分子量

548.06

包装储存

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

生物活性

Edoxaban (DU-176b) is an orally active, highly potent, selective, and direct Factor Xa (FXa) inhibitor with K_i values of 0.561 and 2.98 nM for free human FXa and prothrombinase. Edoxaban exhibits more than 10,000-fold selectivity over other coagulation proteases. Edoxaban can be used in preventing thromboembolic disease research.

性状

Solid

IC50 & Target[1][2]

IC50: 2.90 μM (platelet aggregation), Ki: 0.561 nM (free human FXa), 2.98 nM (prothrombinase), 0.715 nM (cynomolgus monkey FXa), 0.457 nM (rabbit FXa)

体外研究(In Vitro)

Edoxaban (1, 1 and 5 minutes respectively) prolongs PT,TT and APTT of human plasma in a concentration-dependent manner.
Edoxaban inhibits thrombin-induced platelet aggregation, with an IC₅₀ of 2.90 μM.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	Human, rat, cynomolgus monkey and rabbit plasma; Human platelet
Concentration:
Incubation Time:	1 and 5 minutes
Result:	Antithrombin.

体内研究(In Vivo)

Edoxaban (0.5, 2.5 and 12.5 mg/kg; p.o.; once) significantly and dose-dependently reduces the thrombus formation and prolongs PT.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male Slc: Wistar rats (210-240 g); Male New Zealand White rabbits(2.5-3.5 kg) (Both are venous stasis thrombosis model).
Dosage:	0.5, 2.5 and 12.5 mg/kg
Administration:	Oral administration; once
Result:	Inhibited exogenous FXa activity. Antithrombotic.

运输条件

Room temperature or refrigerated transportation.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

ClinicalTrial

参考文献

[1]. Furugohri T, et al. DU-176b, a potent and orally active factor Xa inhibitor: 体外研究 and in vivo pharmacological profiles. J Thromb Haemost. 2008 Sep;6(9):1542-9. [Information]

溶解度数据

体外研究:

DMSO : 10 mg/mL (18.25 mM; Need ultrasonic)

配制储备溶液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8246 mL	9.1231 mL	18.2462 mL
5 mM	0.3649 mL	1.8246 mL	3.6492 mL
10 mM	0.1825 mL	0.9123 mL	1.8246 mL

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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