Indacaterol Maleate (C007B-196332)

InformationIndacaterol (QAB149) is an ultra-long-actingβ-adrenoceptoragonist withpKiof 7.36 for β1-adrenoceptor andpKiof 5.48 for β2-adrenoceptor.In vitroIndacaterol 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 vivoIndacaterol (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 Datacell lines：Concentrations：Incubation Time：Powder Purity:≥99%. Specification: 10mM in DMSO Molecular Formula: C24H28N2O3·C4H4O4 Molecular Weight: 508.56 Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/I408354-SCI_261dd5249ca6dda7de27881d127862d8.pdf