Umeclidinium-d10 bromide(Synonyms: GSK573719A-d10)

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Umeclidinium-d10 bromide (Synonyms: GSK573719A-d10)

Umeclidinium-d10 bromide (GSK573719A-d10) 是 Umeclidinium bromide 的氘代物。Umeclidinium bromide 是一种 mAChR 拮抗剂。Umeclidinium bromide 作用于克隆的人 M1-M5 mAChRs，Ki 为 0.05 到 0.16 nM。

Umeclidinium-d10 bromide(Synonyms: GSK573719A-d10)

Umeclidinium-d10 bromide Chemical Structure

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生物活性

Umeclidinium-d10 bromide (GSK573719A-d10) is the deuterium labeled Umeclidinium bromide. Umeclidinium bromide is a novel mAChR antagonist. The affinity (Ki) of Umeclidinium bromide for the cloned human M1-M5 mAChRs ranges from 0.05 to 0.16 nM.

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

518.55

Formula

C29H24D10BrNO2
中文名称

芜地溴铵 d10 (溴盐)
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]. Salmon M, et al. Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. J Pharmacol Exp Ther. 2013 May;345(2):260-70.

    [3]. Cazzola M, et al. Pharmacology and therapeutics of bronchodilators. Pharmacol Rev. 2012 Jul;64(3):450-504.

    [4]. Calzetta L, et al. Pharmacological characterization of the interaction between umeclidinium and vilanterol in human bronchi. Eur J Pharmacol. 2017 Jul 14. pii: S0014-2999(17)30470-3.

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