Indacaterol Maleate

Modify Date: 2024-01-02 17:06:22

Indacaterol Maleate Structure
Indacaterol Maleate structure
Common Name Indacaterol Maleate
CAS Number 753498-25-8 Molecular Weight 508.563
Density N/A Boiling Point N/A
Molecular Formula C28H32N2O7 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Indacaterol Maleate


Indacaterol Maleate is an ultra-long-acting β-adrenoceptor agonist.Target: β-adrenoceptorIndacaterol 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 (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].

 Names

Name indacaterol maleate
Synonym More Synonyms

 Indacaterol Maleate Biological Activity

Description Indacaterol Maleate is an ultra-long-acting β-adrenoceptor agonist.Target: β-adrenoceptorIndacaterol 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 (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].
Related Catalog
References

[1]. Battram, C., et al., In vitro and in vivo pharmacological characterization of 5-[(R)-2-(5,6-diethyl-indan-2-ylamino)-1-hydroxy-ethyl]-8-hydroxy-1H-quinolin-2-o ne (indacaterol), a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action. J Pharmacol Exp Ther, 2006. 317(2): p. 762-70.

[2]. Sturton, R.G., et al., Pharmacological characterization of indacaterol, a novel once daily inhaled 2 adrenoceptor agonist, on small airways in human and rat precision-cut lung slices. J Pharmacol Exp Ther, 2008. 324(1): p. 270-5.

 Chemical & Physical Properties

Molecular Formula C28H32N2O7
Molecular Weight 508.563
Exact Mass 508.220947
PSA 160.21000
LogP 3.66390
Storage condition 2~8℃

 Safety Information

Hazard Codes Xi

 Synonyms

QAB-149 maleate
Indacaterolmaleate
UNII-2JEC1ITX7R
Onbrez Breezhaler
Arcapta neohaler
Hirobriz Breezhaler
5-{(1R)-2-[(5,6-Diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl}-8-hydroxy-2(1H)-quinolinone (2Z)-2-butenedioate (1:1)
2(1H)-Quinolinone, 5-[(1R)-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy-, (2Z)-2-butenedioate (1:1) (salt)
(Z)-but-2-enedioic acid,5-[(1R)-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one
Indacaterol Maleate
Oslif Breezhaler
Indacaterol (maleate)
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