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- 详细信息
- 文献和实验
- 技术资料
- 保存条件：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 保质期：
Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year
- 英文名：
Indacaterol Maleate
- 库存：
现询
- 供应商：
北京索莱宝科技有限公司
- CAS号：
753498-25-8
- 规格：
500mg/100mg
| 规格： | 500mg | 产品价格： | ￥4918.0 |
|---|---|---|---|
| 规格： | 100mg | 产品价格： | ￥1758.0 |
| 基本信息 | |
| CAS | No.753498-25-8 |
| 中文名称 | 马来酸茚达特罗 |
| 英文名称 | Indacaterol Maleate |
| 别名 | QAB149 |
| 分子式 | C28H32N2O7 |
| 分子量 | 508.56 |
| 溶解性 | Soluble in DMSO ≥10mg/mL |
| 纯度 | ≥98% |
| 外观(性状) | White to off-white Solid |
| 储存条件 | Powder:2-8℃，2 years;Insolvent(母液):-20℃，6 months;-80℃，1 year |
| MDL | MFCD20526769 |
| 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 |
| InChIKey | IREJFXIHXRZFER-PCBAQXHCSA-N |
| InChI | InChI=1S/C24H28N2O3.C4H4O4/c1-3-14-9-16-11-18(12-17(16)10-15(14)4-2)25-13-22(28)19-5-7-21(27)24-20(19)6-8-23(29)26-24;5-3(6)1-2-4(7)8/h5-10，18，22，25，27-28H，3-4，11-13H2，1-2H3，(H，26，29);1-2H，(H，5，6)(H，7，8)/b;2-1-/t22-;/m0./s1 |
| PubChem CID | 9827599 |
| 靶点 | Adrenergic Receptor |
| 通路 | Endocrinology & Hormones;GPCR & G Protein；Neuronal Signaling |
| 背景说明 | 是一种长效β-ADr受体激动剂。 |
| 生物活性 | Indacaterol Maleate 是一种长效的β-ADr受体激动剂，对β1-adrenoceptor的pKi为 7.36，对 β2-adrenoceptor 的pKi为5.48，可以用于治疗哮喘和慢性阻塞性肺病。[1] |
| In Vitro | Indacaterol is close to a full agonist at the human beta(2)adrenoceptor(E(max)= 73 +/- 1% of the maximal effect of isoprenaline; pEC(50)= 8.06 +/- 0.02).[1] Indacaterol as a fast acting compound with a longer duration of action than salmeterol and formoterol.[2] Duration of action was determined against cholinergic neural contraction induced by electrical field stimulation(EFS). At resting tone，-logEC50 and Emax values were 8.82+/-0.41 and 77+/-5% for indacaterol. Indacaterol's onset of action(7.8+/-0.7 min) was significantly faster than that of salmeterol(19.4+/-4.3 min). EFS-induced contractions were inhibited with -logIC50 values of 6.96+/-0.13(indacaterol). Duration of action was >12 h for indacaterol and salmeterol.[3] Indacaterol is an effective inhibitor of the release of mediators from human lung mast cells. Indacaterol was as potent and as efficacious as the full agonist，isoprenaline(EC(50)，approximately 4 nmol x L(-1))，at inhibiting the IgE-dependent release of histamine from mast cells.[4] In both the low- and high-expression recombinant GEVT 'wild type' cell lines indacaterol is a high-efficacy agonist. In the human primary ASM cells indacaterol gave a maximal response intermediate between that of salmeterol and formoterol.[5] |
| 细胞实验 | In isolated superfused guinea pig trachea，indacaterol has a fast onset of action(30 +/- 4 min)and a long duration of action(529 +/- 99 min). In the conscious guinea pig，when given intratracheally as a dry powder，indacaterol inhibits 5-hydroxytryptamine-induced bronchoconstriction for at least 24 h，whereas salmeterol，formoterol，and salbutamol have durations of action of 12，4，and 2 h，respectively.[1] |
| 数据来源文献 | [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-one (indacaterol)，a novel inhaled beta(2) adrenoceptor agonist with a 24-h duration of action. J Pharmacol Exp Ther. 2006 May;317(2):762-70. [2]. Sturton RG，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 Jan;324(1):270-5. [3]. Naline E，et al. Effect of indacaterol，a novel long-acting beta2-agonist，on isolated human bronchi. Eur Respir J. 2007 Mar;29(3):575-81. [4]. Scola AM，et al. The long-acting beta-adrenoceptor agonist，indacaterol，inhibits IgE-dependent responses of human lung mast cells. Br J Pharmacol. 2009 Sep;158(1):267-76. [5]. Sayers I，et al. Pharmacogenetic characterization of indacaterol，a novel beta 2-adrenoceptor agonist. Br J Pharmacol. 2009 Sep;158(1):277-86. |
| 单位 | 瓶 |
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