马来酸茚达特罗 T1239

Product Introduction
Bioactivity


英文名: Indacaterol maleate

描述: Indacaterol maleate (QAB149) 是一种超长效的 β-肾上腺素受体激动剂。

体外活性: 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. [1] 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. [2] Indacaterol (10 μM) induces close to full inhibition of the EFS-induced contraction of isolated human bronchi and the effect lasts 12 hours. [3] 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. [4] 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. [5]

体内活性: 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. [1]

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度: DMSO : 94 mg/mL (184.8 mM)
Ethanol : < 1 mg/mL (insoluble or slightly soluble)


关键字: Inhibitor | NF-κB | heart failure | Indacaterol maleate | myocardial infarction | Adrenergic Receptor | Indacaterol Maleate | asthma | QAB-149 | HT1080 cells | QAB 149 | inhibit | Indacaterol | COPD | β-arrestin2 | Beta Receptor

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相关库: Anti-Neurodegenerative Disease Compound Library | Drug Repurposing Compound Library | Anti-Cancer Drug Library | Membrane Protein-targeted Compound Library | Neuronal Signaling Compound Library | GPCR Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Approved Drug Library | EMA Approved Drug Library | Bioactive Compound Library

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