Indacaterol maleate

SKU: orb1309276

Description

Indacaterol maleate

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	753498-25-8
MW	508.56
Purity	99.67%
Formula	C₂₈H₃₂N₂O₇
SMILES	OC(=O)\C=C/C(O)=O.CCc1cc2CC(Cc2cc1CC)NC[C@H](O)c1ccc(O)c2[nH]c(=O)ccc12
Target	Adrenergic Receptor
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.93 mM);DMSO:94 mg/mL (184.84 mM);Ethanol:< 1 mg/mL (insoluble or slightly soluble)

Bioactivity

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Target IC50	β2-adrenoceptor:5.48(pKi)\|β1-adrenoceptor:7.36(pKi)
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. Read more...
In Vitro	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 o 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 reverse the carbachol-induced contraction in a concentration dependent manner with IC50 of 37 nM in human s All airways. Indacaterol concentration dependently reverse the serotonin-induced contraction with IC50 of 10.5 nM in rat s All airways. Indacaterol ha the highest intrinsic efficacy of 53% in rat s All airways and 73% in human s All airways. Indacaterol (10 μM) induces close to full Inhibition o the EFS-induced contraction of isolated human bronchi an the effect lasts 12 hours. Indacaterol inhibit the IgE-dependent release of histamine from mast cells wit the intrinsic activity (Emax of a long-acting Indacaterol/Emax of Isoprenaline) of 1.03. Indacaterol inihbits cAMP release from human airway smooth musclee with pEC50 of 8.53 and Emax of 48%. Indacaterol appears to have a reduced efficacy compared wit the CHO-K1 data in the Primary ASM cells. Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Disclaimer	For research use only

Alternative Names

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COPD, Beta Receptor, AdrenergicReceptor, Adrenergic Receptor, asthma, HT1080 cells, heart failure, inhibit, Inhibitor, myocardial infarction, Indacaterol, Indacaterol maleate, Indacaterol Maleate, NF-κB, β1-adrenoceptor, β2-adrenoceptor, β-arrestin2, QAB149, QAB-149, QAB 149

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Compound Identifiers

PubChem CID

9827599 ↗

Key Properties

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No computed properties available.

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