Dabigatran ethyl ester-d3 hydrochloride

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Dabigatran ethyl ester-d3 hydrochloride 

Dabigatran ethyl ester-d3 hydrochloride 是 Dabigatran (ethyl ester hydrochloride) 的氘代物。Dabigatran ethyl ester hydrochloride是有效地核糖基二氢烟酰胺脱氢酶(NQO2)抑制剂,IC50值为0.8 μM;也是凝血酶的抑制剂。

Dabigatran ethyl ester-d3 hydrochloride

Dabigatran ethyl ester-d3 hydrochloride Chemical Structure

CAS No. : 2469244-68-4

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生物活性

Dabigatran ethyl ester-d3 hydrochloride is the deuterium labeled Dabigatran (ethyl ester hydrochloride). Dabigatran ethyl ester hydrochloride is a potent inhibitor of ribosyldihydronicotinamide dehydrogenase (NQO2) with an IC50 value of 0.8 μM and a thrombin inhibitor.

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

539.04

Formula

C27H27D3ClN7O3

CAS 号

2469244-68-4

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]. Michaelis S, et al. Dabigatran and dabigatran ethyl ester: potent inhibitors of ribosyldihydronicotinamide dehydrogenase (NQO2). J Med Chem. 2012 Apr 26;55(8):3934-44.

    [3]. Eisert WG, et al. Dabigatran: an oral novel potent reversible nonpeptide inhibitor of thrombin. Arterioscler Thromb Vasc Biol. 2010 Oct;30(10):1885-9.

    [4]. Hauel NH, et al. Structure-based design of novel potent nonpeptide thrombin inhibitors. J Med Chem. 2002 Apr 25;45(9):1757-66.

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