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Olodaterol

SKU: orb2276859

Description

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.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Images & Validation

Key Properties

CAS Number868049-49-4
MW386.45
Purity98.00%
FormulaC21H26N2O5
SMILESCOc1ccc(CC(C)(C)NC[C@H](O)c2cc(O)cc3NC(=O)COc23)cc1
TargetAdrenergic Receptor
Solubility10% DMSO+40% PEG300+5% Tween-80+45% Saline:1 mg/mL (2.59 mM);DMSO:10 mM

Bioactivity

Target IC50
β2-adrenoceptor:0.1 nM (EC50)
In Vivo
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. 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.
In Vitro
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.
Cell Research
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.

Storage & Handling

Storagestore at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

Beta Receptor, COPD, Adrenergic Receptor, AdrenergicReceptor, BI 1744, BI1744, BI-1744, Fibrosis, Inhibitor, Inhaled, inhibit, Olodaterol, Long-acting, Striverdi Respimat, Potent, Ultra-LABA, β2-adrenoceptor

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Key Properties

No computed properties available.

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Olodaterol (orb2276859)

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% Tween 80 +
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1 mg
¥ 1,170.00
5 mg
¥ 3,120.00
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