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Indacaterol Maleate
本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。
Indacaterol Maleate图片
CAS NO:753498-25-8
包装与价格：
包装价格(元)
5mg电议
50mg电议

产品介绍
马来酸茚达特罗 (QAB149) 是一种具有口服活性的超长效 β2 肾上腺素受体 (ADRB2) 激动剂。
Cas No.753498-25-8
别名马来酸茚达特罗; QAB149
化学名(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
Canonical SMILESCCC1=C(C=C2CC(CC2=C1)NCC(C3=C4C=CC(=O)NC4=C(C=C3)O)O)CC.C(=CC(=O)O)C(=O)O
分子式C24H28N2O3.C4H4O4
分子量508.56
溶解度≥ 51.6 mg/mL in DMSO, ≥ 10.02 mg/mL in ETOH with gentle warming
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

Indacaterol (QAB149) maleate is an ultra-long-acting β-adrenoceptor agonist.

Indacaterol (QAB149) inhibits cAMP production in Chinese hamster ovary cells stably transfected with human β2 adrenoceptors with pEC50 of 8.06. Indacaterol (QAB149) 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 (QAB149) (6.7 μg/kg) inhibits 5-HT-induced bronchoconstriction with a maximal effect of 85% in the conscious guinea pig. Indacaterol (QAB149) (12.5 μg/kg) dose-dependently inhibits methacholine-induced bronchoconstriction with a maximal effect of 85% in the anesthetized rhesus monkey[1].

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.