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Cited in 0 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
Indacaterol (QAB149) is an ultra-long-actingβ-adrenoceptoragonist withpKiof 7.36 for β1-adrenoceptor andpKiof 5.48 for β2-adrenoceptor.
In vitro
Indacaterol induces cAMP production in Chinese hamster ovary cells stably transfected with human β2 adrenoceptors. It 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 induces cAMP production 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.
In vivo
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.
Cell Data
cell lines:
Concentrations:
Incubation Time:
Powder Purity:≥99%
| Isomeric SMILES | CCC1=C(C=C2CC(CC2=C1)NC[C@@H](C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC.C(=C\C(=O)O)\C(=O)O |
|---|---|
| PubChem CID | 9827599 |
| Molecular Weight | 508.57 |
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View spec sheet →| Solubility | Solubility (25°C) In vitro |
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