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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 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。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 343 | 期货 | |
5 mg | ¥ 728 | 期货 |
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 |
分子量 | 386.45 |
分子式 | C21H26N2O5 |
CAS No. | 868049-49-4 |
Smiles | COc1ccc(CC(C)(C)NC[C@H](O)c2cc(O)cc3NC(=O)COc23)cc1 |
密度 | 1.250 g/cm3 |
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 | |||||||||||||||||||||
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