Olodaterol

SKU: orb2276859

Description

Olodaterol is a long-acting beta2-adrenergic agonist (LABA) designed for selective activation of pulmonary beta2-adrenergic receptors. It is widely used in respiratory research, including in vitro receptor studies and in vivo models of bronchoconstriction, such as chronic obstructive pulmonary disease (COPD).

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 868049-49-4
• MW: 386.45
• Purity: 98.90% (May vary between batches)
• Formula: C₂₁H₂₆N₂O₅
• SMILES: COc1ccc(CC(C)(C)NC[C@H](O)c2cc(O)cc3NC(=O)COc23)cc1
• Target: Adrenergic Receptor
• Solubility: 10% 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

• Storage: store 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 Date: 12 months from date of receipt.
• Disclaimer: For 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

Compound Identifiers

PubChem CID

11504295