Umeclidinium bromide

- Overview
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    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].
    
    [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.
- Properties
  - Categories
    
    MAChR antagonist
    
    Alternative Name
    
    GSK573719A;GSK-573719A;GSK 573719A; diphenyl-[1-(2-phenylmethoxyethyl)-1-azoniabicyclo[2.2.2]octan-4-yl]methanol;bromide
    
    CAS Number
    
    869113-09-7
    
    Molecular Formula
    
    C29H34BrNO2
    
    Molecular Weight
    
    508.49
    
    Purity
    
    98.00%
    
    Solubility
    
    insoluble in H2O; insoluble in EtOH; ≥61.5 mg/mL in DMSO
    
    Storage
    
    Store at -20°C
    
    SMILES
    
    C1C[N+]2(CCC1(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)CCOCC5=CC=CC=C5.[Br-]
    
    * For Research Use Only

Documents

COA (Certificate Of Analysis)

MSDS (Material Safety Data Sheet)

Datasheet

Umeclidinium bromide

Background

Documents

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