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Umeclidinium bromide

Chemical Structure : Umeclidinium bromide

CAS No.: 869113-09-7

Umeclidinium bromide (GSK573719A, GSK573719A)

Catalog No.: PC-42894Not For Human Use, Lab Use Only.

Umeclidinium bromide (GSK573719A) is potent, long-acting, inhaled antagonist of mAChRs with Ki of 0.05-0.16 nM for human M1-M5 mAChRs.

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Biological Activity

Umeclidinium bromide (GSK573719A) is potent, long-acting, inhaled antagonist of mAChRs with Ki of 0.05-0.16 nM for human M1-M5 mAChRs.
Umeclidinium bromide demonstrates picomolar potency (-log pA2=23.9 pM) in an acetylcholine-mediated Ca(2+) mobilization assay in CHO cells transfected M3 mAChRs.
Umeclidinium bromide dose dependently blocks Ach-induced bronchoconstriction with long duration of action in mice model of pulmonary diseases.

Physicochemical Properties

M.Wt 508.4897
Formula C29H34BrNO2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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Solubility

DMSO: ≥ 34 mg/mL

Chemical Name/SMILES

1-Azoniabicyclo[2.2.2]octane, 4-(hydroxydiphenylmethyl)-1-[2-(phenylmethoxy)ethyl]-, bromide (1:1)

References

1. Salmon M, et al. J Pharmacol Exp Ther. 2013 May;345(2):260-70.

2. Tal-Singer R, et al. Eur J Pharmacol. 2013 Feb 15;701(1-3):40-8.

3. Decramer M, et al. Respir Physiol Neurobiol. 2013 Jan 15;185(2):393-9.

4. Decramer M, et al. Lancet Respir Med. 2014 Jun;2(6):472-86.

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