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Olodaterol

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产品编号 T3457Cas号 868049-49-4
别名 Striverdi Respimat, BI1744

Olodaterol 是一种长效的、选择性 β2-adrenoceptor(β2-AR) 激动剂 (EC50=0.1 nM;pKi= 9.14 for human β2-adrenoceptor),可用于慢性阻塞性肺疾病 (COPD) 和肺纤维化的研究。

Olodaterol

Olodaterol

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纯度: 98.9%
产品编号 T3457 别名 Striverdi Respimat, BI1744Cas号 868049-49-4

Olodaterol 是一种长效的、选择性 β2-adrenoceptor(β2-AR) 激动剂 (EC50=0.1 nM;pKi= 9.14 for human β2-adrenoceptor),可用于慢性阻塞性肺疾病 (COPD) 和肺纤维化的研究。

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1 mg¥ 343期货
5 mg¥ 728期货
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产品介绍

生物活性
产品描述
Olodaterol is a novel, long-acting beta2-adrenergic agonist (LABA) that exerts its pharmacological effect by binding and activating beta2-adrenergic receptors located primarily in the lungs.
靶点活性
β2-adrenoceptor:0.1 nM (EC50)
体外活性
Olodaterol shows a potent, nearly full agonistic response at the hβ2-adrenoceptor (EC50=0.1 nM; intrinsic activity=88% compared with isoprenaline) and a significant selectivity profile (241- and 2299-fold against the hβ1- and hβ3-ARs, respectively). Likewise, olodaterol is able to potently reverse contraction induced by different stimuli in isolated human bronchi[2].
体内活性
Olodaterol is a long acting β2-agonist that induces bronchodilation up to 24 h after dosing in patients with chronic obstructive pulmonary disease (COPD) . Olodaterol dose-dependently attenuates cell influx and pro-inflammatory mediator release in murine and guinea pig models of pulmonary inflammation. Olodaterol attenuates pro-inflammatory mediator release from human parenchymal explants and whole blood and reduced expression of CD11b adhesion molecules on granulocytes, but without direct effects on IL-8-induced neutrophil transwell migration[3]. Once-daily olodaterol 5 μg is an effective therapy in improving lung function and symptomatic outcomes in patients with moderate to very severe (COPD) receiving other maintenance therapy, with a satisfactory safety profile[4].
细胞实验
To determine the functional potency of the different agonists against the different hβ-ARs, changes in intracellular cAMP levels are determined with CHO cells in suspension and a 384-well plate format. In brief, cells are stimulated with the respective agonists at different concentrations in Hanks' buffered saline solution. Cells are lysed by using Alphascreen reagents. After 2 h, plates are read on an Envision plate reader. The concentration of cAMP in the samples is calculated from a standard curve[2].
别名Striverdi Respimat, BI1744
化学信息
分子量386.45
分子式C21H26N2O5
CAS No.868049-49-4
SmilesCOc1ccc(CC(C)(C)NC[C@H](O)c2cc(O)cc3NC(=O)COc23)cc1
密度1.250 g/cm3
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
DMSO: 10 mM
溶液配制表
1mg5mg10mg50mg
1 mM2.5877 mL12.9383 mL25.8766 mL129.3828 mL
5 mM0.5175 mL2.5877 mL5.1753 mL25.8766 mL
10 mM0.2588 mL1.2938 mL2.5877 mL12.9383 mL

计算器

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体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
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2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
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