Umeclidinium-d10 (bromide)
Umeclidinium-d10 (bromide) 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.
Product Specifications
Product Name Alternative
GSK573719A-d10
UNSPSC
12352005
Target
MAChR
Type
Isotope-Labeled Compounds
Related Pathways
GPCR/G Protein; Neuronal Signaling
Field of Research
Inflammation/Immunology
Solubility
10 mM in DMSO
Smiles
OC(C1=C([2H])C([2H])=C([2H])C([2H])=C1[2H])(C23CC[N+](CC2)(CC3)CCOCC4=CC=CC=C4)C5=C([2H])C([2H])=C([2H])C([2H])=C5[2H].[Br-]
Molecular Formula
C29H24D10BrNO2
Molecular Weight
518.55
References & Citations
[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.
Shipping Conditions
Room temperature
Scientific Category
Isotope-Labeled Compounds
Clinical Information
No Development Reported
Isoform
MAChR1; mAChR5
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