Vilanterol

Cat. No. :	HY-14300
M.Wt:	486.43
Formula:	C24H33Cl2NO5
Purity:	>98 %
Solubility:

Introduction of 503068-34-6 :

Vilanterol (GW642444) is a long-acting β₂ adrenergic receptor agonist. Vilanterol has pEC₅₀ values for β₂-AR, β₁-AR, and β₃-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol selectively activates airway β₂ adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol can be used in asthma research^[3][5]. IC50 & Target:pEC50: 10.37±0.05 (β₂-adrenoceptor), 6.98±0.03 (β₁-adrenoceptor), 7.36±0.03 (β₃-adrenoceptor)^[1] In Vitro:

Vilanterol (Compound 13f) is a highly efficient (β₂: pEC₅₀ = 9.4), highly active (IA = 0.69), and highly selective (pEC₅₀ difference: β₂/β₁ = 3.0) β₂ receptor agonist in CHO cells transfected with human β₁, β₂, and β₃ receptors^[5].

Vilanterol (5 μM, 30 min) undergoes rapid metabolic inactivation in the systemic circulation during human liver microsome experiments^[5].

Vilanterol has moderate membrane permeability in MDCKII-MDR1 cells (P_app = 34 nm/s), which may reduce systemic absorption^[5].

Vilanterol is highly selective for β₂-AR, with at least 1000-fold selectivity for the β₂-AR and β₃-AR subtypes^[3].

In Vivo:Vilanterol (Compound 13f) (30 μM, 300 μM, Nebulizer inhalation, Once dose) exerts a long-lasting effect on in vivo bronchial dilation following inhalation. The higher the administered dose, the longer the duration of this effect, and it can significantly alleviate asthma symptoms in histamine-induced bronchospasm in the guinea pig^[5].