Vilanterol (GW642444) acetate is a long-acting β2-AR agonist. The pEC50 values for vilanterol acetate are 9.4 for β2-AR, 6.4 for β1-AR, and 6.1 for β3-AR, indicating its selectivity in activating airway β2-AR receptors. This activation elevates cAMP levels, resulting in the relaxation of bronchial smooth muscle. Vilanterol acetate can be used in asthma-related research.

Vilanterol acetate (Compound 13f) is a potent and highly active β2 receptor agonist, demonstrating high selectivity (pEC50 difference: β2/β1 = 3.0) in CHO cells transfected with human β1, β2, and β3 receptors, with a pEC50 of 9.4 and an intrinsic activity (IA) of 0.69. In human liver microsome assays, it undergoes rapid metabolic inactivation in systemic circulation when used at 5 μM for 30 minutes. The compound exhibits moderate membrane permeability (P_app = 34 nm/s) in MDCKII-MDR1 cells, which may result in reduced systemic absorption. Furthermore, Vilanterol acetate has a selectivity for β2-AR over β3-AR subtypes that is at least 1000-fold greater.

Vilanterol acetate (Compound 13f) exhibited a sustained bronchodilatory effect when inhaled by nebulization at doses of 30 μM and 300 μM. After a single nebulization administration, this compound effectively prolonged the duration of action and significantly alleviated the asthma symptoms in guinea pigs with histamine-induced bronchospasm. The higher the dose, the more pronounced the effect.