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Umeclidinium bromide
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Umeclidinium bromide图片
CAS NO:869113-09-7
规格:98%
分子量:508.49
包装与价格:
包装价格(元)
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
MAChR antagonist
CAS:869113-09-7
分子式:C29H34BrNO2
分子量:508.49
纯度:98%
存储:Store at -20°C

Background:

Umeclidinium bromide is a potent and long-acting antagonist of muscarinic cholinergic receptor (mAChR) with Ki values of 0.16nM, 0.15nM, 0.06nM, 0.05nM and 0.13nM for M1, M2, M3, M4 and M5, respectively [1].


Umeclidinium bromide is developed for the treatment of chronic obstructive pulmonary disease (COPD). It can help patients of COPD achieve sufficient oxygenation of extrapulmonary tissues through dilating the airways. In the in vitro assay, umeclidinium binds to recombinant human mAChRs with Ki value of 0.16nM, 0.15nM, 0.06nM, 0.05nM and 0.13nM for M1-M5, respectively. Umeclidinium is selective against mAChR over other unrelated receptors or channels such as κ and σ opiod receptors, Na+ channel and dopamine transporter. In CHO cells transfected with human recombinant mAChRs, umeclidinium affects the calcium flux responsed to Ach with pA2 values of 9.6-10.6 for M1-M3. In a murine model, administration of umeclidinium can reverse the bronchoconstriction caused by Ach [1].


参考文献:
[1] Salmon M, Luttmann M A, Foley J J, et al. Pharmacological characterization of GSK573719 (umeclidinium): a novel, long-acting, inhaled antagonist of the muscarinic cholinergic receptors for treatment of pulmonary diseases. Journal of Pharmacology and Experimental Therapeutics, 2013, 345(2): 260-270.