Home Neuronal Signaling Adrenergic Receptor agonist Indacaterol Maleate For research use only.

Indacaterol Maleate

Synonyms: QAB149

Indacaterol (QAB149) is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36 for β1-adrenoceptor and pKi of 5.48 for β2-adrenoceptor.

Indacaterol Maleate Chemical Structure

Indacaterol Maleate Chemical Structure

CAS: 753498-25-8

Selleck's Indacaterol Maleate has been cited by 1 publication

Purity & Quality Control

Batch: S308301 DMSO] 102 mg/mL] false] Water] Insoluble] false] Ethanol] Insoluble] false Purity: 99.88%
99.88

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Biological Activity

Description Indacaterol (QAB149) is an ultra-long-acting β-adrenoceptor agonist with pKi of 7.36 for β1-adrenoceptor and pKi of 5.48 for β2-adrenoceptor.
Targets
β1-adrenoceptor [1] β2-adrenoceptor [1]
7.36(pKi) 5.48(pKi)
In vitro
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. [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 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. [5]
In Vivo
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. [1]
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05288075 Completed Healthy Volunteers Orion Corporation Orion Pharma February 28 2022 Phase 1
NCT03030638 Completed Pulmonary Disease Chronic Obstructive Boehringer Ingelheim|RTI health solutions US February 8 2017 --

Chemical lnformation & Solubility

Molecular Weight 508.56 Formula

C24H28N2O3.C4H4O4
CAS No. 753498-25-8 SDF Download Indacaterol Maleate SDF
Smiles CCC1=C(C=C2CC(CC2=C1)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC.C(=CC(=O)O)C(=O)O
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 102 mg/mL ( (200.56 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Water : Insoluble

Ethanol : Insoluble


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In vivo
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