计算溶液所需的质量、体积或浓度。
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在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
Indacaterol (QAB149)是一种超长效的β-adrenoceptor激动剂,对β1-adrenoceptor的pKi为 7.36,对 β2-adrenoceptor 的pKi为5.48。
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%
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
| 分析证书 | I408354 |