Dabigatran-d4(Synonyms: BIBR 953-d4; BIBR 953ZW-d4)

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Dabigatran-d4 (Synonyms: BIBR 953-d4; BIBR 953ZW-d4)

Dabigatran-d4 是 Dabigatran 氘代物。Dabigatran (BIBR 953),口服抗凝剂,是可逆的,竞争性的直接凝血酶 (thrombin) 抑制剂,Ki 为 4.5 nM。Dabigatran (BIBR 953) 也抑制凝血酶诱导的血小板聚集 (IC50=10 nM)。

Dabigatran-d4(Synonyms: BIBR 953-d4;  BIBR 953ZW-d4)

Dabigatran-d4 Chemical Structure

CAS No. : 1618637-32-3

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生物活性

Dabigatran-d4 is deuterium labeled Dabigatran. Dabigatran (BIBR 953), an oral anticoagulant, is a reversible, potent, competitive direct thrombin inhibitor (Ki=4.5 nM). Dabigatran (BIBR 953) also inhibits thrombin-induced platelet aggregation (IC50=10 nM)[1][2].

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

475.54

Formula

C25H21D4N7O3

CAS 号

1618637-32-3

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

    [3]. Wienen W, Stassen JM, Priepke H, In-vitro profile and ex-vivo anticoagulant activity of the direct thrombin inhibitor dabigatran and its orally activeprodrug, dabigatran etexilate. Thromb Haemost. 2007 Jul;98(1):155-62.

    [4]. Wienen W, et al. Effects of the direct thrombin inhibitor dabigatran and its orally active prodrug, dabigatran etexilate, on thrombus formation and bleeding time in rats. Thromb Haemost. 2007 Aug;98(2):333-8.

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