Indacaterol maleate|753498-25-8|(马来酸茚达特罗; QAB149)-陌孚医药/Medlife

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Indacaterol maleate (Synonyms: 马来酸茚达特罗; QAB149)

目录号: PL14305 纯度: ≥99%

CAS No. :753498-25-8

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中文名称	Indacaterol maleate
中文别名	马来酸茚达特罗;茚达特罗马来酸盐;Indacaterol Maleate 茚达特罗马来酸盐;茚达特罗;印达特罗中间体
英文名称	Indacaterol maleate
英文别名	Indacaterol Maleate;Indacaterol Maleic Acid 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;QAB149;Arcapta;Onbrez;QAB 149;(R)-5-(2-(5,6-diethyl-2,3-dihydro-1H-inden-2-ylamino)-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one;8OR09251MQ;5-[(1R)-2-[(5,6-diethyl-2,3-dihydro-1H-inden-2-yl)amino]-1-hydroxyethyl]-8-hydroxy-1H-quinolin-2-one;Indacaterol (USAN/INN);Indacaterol [USAN:INN:BAN];5-{(1R)-2-((5,6-Diethyl-2,3-dihydro-1H-inden-2-yl)amino)-1-hydroxyethyl}-8-hydroxyquinolin-2(1H;Indacaterol maleate
Cas No.	753498-25-8
分子式	C₂₄H₂₈N₂O₃
分子量	392.49
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

产品详情

Indacaterol maleate (QAB149) 是一种口服有效的超长效 ADRB2 激动剂。Indacaterol maleate 能以 β-arrestin2 依赖的方式抑制 NF-κB 活性，防止进一步的肺部损伤，并改善慢性阻塞性肺病 (COPD) 的肺功能。Indacaterol maleate 还可用于心血管疾病的研究。

生物活性

Indacaterol maleate (QAB149) is an orally active ultra-long-acting β2 adrenergic receptor (ADRB2) agonist. Indacaterol maleate inhibits NF-κB activity in a β-arrestin2-dependent manner, preventing further lung damage and improving lung function in COPD (chronic obstructive pulmonary disorder). Indacaterol maleate can also be used in cardiovascular disease research.

性状

Solid

IC50 & Target[1][2]

β-adrenoceptor β adrenergic receptor

体外研究(In Vitro)

Indacaterol maleate (1, 2.5, 5, 10 μM; 12 h) inhibits TNF-α induced MMP-9 expression and activity in human fibrosarcoma HT1080 cells.
Indacaterol maleate (10 μM; 6 h) inhibits TNF-α induced invasion and migration of human fibrosarcoma cells by reducing MMP-9 expression and activity.
Indacaterol maleate (1, 2.5, 5, 10 μM; 2.5 h) inhibits TNF-α-activated IKK/NF-кB signaling in HT1080 cells. has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

Indacaterol maleate (0.3 mg/kg; in animal drinking water; sinle daily for 15 weeks) shows activity of normalizing and reversing cardiac remodeling in a myocardial infarction (MI) rat model of heart failure (HF). has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model:

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

参考文献

[1]. Lee SU, et al. Indacaterol inhibits tumor cell invasiveness and MMP-9 expression by suppressing IKK/NF-κB activation. Mol Cells. 2014 Aug;37(8):585-91.
[2]. Calzetta L, et al. Effects of the new ultra-long-acting β2-AR agonist indacaterol in chronic treatment alone or in combination with the β1-AR blocker metoprolol on cardiac remodelling. 2015.

溶解度数据	In Vitro: DMSO : 100 mg/mL (196.63 mM; Need ultrasonic)H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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