Edoxaban-d6(Synonyms: DU-176-d6)

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白、同位素标记物,专注于信号通路和疾病研究领域。
Edoxaban-d6 (Synonyms: DU-176-d6)

Edoxaban-d6 是 Edoxaban 氘代物。Edoxaban (DU-176) 是一种选择性,有效和口服活性的 factor Xa (FXa) 抑制剂,对游离 FXa 和凝血酶原的 Ki 分别为 0.561 nM 和 2.98 nM。Edoxaban 是一种抗凝剂,可用于预防中风。Edoxaban 还是一种凝血酶和凝血因子 IXaβ (FIXa) 的弱抑制剂,Ki 值分别为 6.00 μM 和 41.7 μM,对 FXa 的选择性超过 10000 倍。Edoxaban 具有抗血栓形成的特性,可用于血栓栓塞性疾病的研究。

Edoxaban-d6(Synonyms: DU-176-d6)

Edoxaban-d6 Chemical Structure

CAS No. : 1304701-57-2

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生物活性

Edoxaban-d6 is deuterium labeled Edoxaban. Edoxaban (DU-176) is a selective, potent and orally active factor Xa (FXa) inhibitor with Kis of 0.561 nM and 2.98 nM for free FXa and prothrombinase, respectively. Edoxaban is an anticoagulant agent and can be used for stroke prevention. Edoxaban is a also weak inhibitor of thrombin and factor IXaβ (FIXa), with Kis of 6.00 μM and 41.7 μM, respectively, exhibits >10 000-fold selectivity for FXa. Edoxaban has antithrombotic properties and has potential for thromboembolic diseases treatment[1][2][3].

体外研究
(In Vitro)

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

554.09

Formula

C24H24D6ClN7O4S

CAS 号

1304701-57-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.

参考文献
  • [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.

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

    [3]. Mendell J, Lee F, Chen S, The Effects of the Antiplatelet Agents, Aspirin and Naproxen, on Pharmacokinetics and Pharmacodynamics of the Anticoagulant Edoxaban, a Direct Factor Xa Inhibitor. J Cardiovasc Pharmacol. 2013 Apr 23. [Epub ahead of print]

    [4]. Stacy ZA, et al. Edoxaban: A Comprehensive Review of the Pharmacology and Clinical Data for the Management of Atrial Fibrillation and Venous Thromboembolism. Cardiol Ther. 2016 Jun;5(1):1-18.

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