Indacaterol Maleate

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Molecular Weight: 508.56 Indacaterol is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36.

Biological Activity

Indacaterol inhibits cAMP production in Chinese hamster ovary cells
stably transfected with human β2 adrenoceptors with pEC50 of 8.06.
Indacaterol inhibits electrically induced contraction on the
electrically stimulated guinea pig trachea in a concentration-dependent
manner with pEC50 of 8.23. Indacaterol induces a concentration-dependent
inotropic effect with maximal efficacy of 75% in the isolated guinea
pig left atrium. Indacaterol reverses the
carbachol-induced contraction in a concentration-dependent manner with
IC50 of 37 nM in human small airways. Indacaterol concentration
dependently reverses the serotonin-induced contraction with IC50 of 10.5
nM in rat small airways.


Indacaterol has the highest intrinsic efficacy
of 53% in rat small airways and 73% in human small airways. Indacaterol (10 μM) induces close to full inhibition of the EFS-induced
contraction of isolated human bronchi and the effect lasts 12 hours. Indacaterol inhibits the IgE-dependent release of histamine from mast
cells with the intrinsic activity (Emax of a long-acting
Indacaterol/Emax of Isoprenaline) of 1.03. Indacaterol
inihbits cAMP release from human airway smooth muscle with pEC50 of 8.53
and Emax of 48%. Indacaterol appears to have a reduced efficacy
compared with the CHO-K1 data in the primary ASM cells.


Indacaterol (6.7 μg/kg) inhibits 5-HT-induced bronchoconstriction with a
maximal effect of 85% in the conscious guinea pig. Indacaterol (12.5
μg/kg) dose-dependently inhibits methacholine-induced
bronchoconstriction with a maximal effect of 85% in the anesthetized
rhesus monkey.

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Product Categories : Neuronal Signaling > Adrenergic Receptor Inhibitor