Vilanterol (trifenatate)

Cat. No. :	HY-14300A
M.Wt:	774.77
Formula:	C44H49Cl2NO7
Purity:	>98 %
Solubility:

Introduction of 503070-58-4 :

Vilanterol (GW642444) trifenatate is a long-acting β₂ adrenergic receptor agonist. Vilanterol trifenatate has pEC₅₀ values for β₂-AR, β₁-AR, and β₃-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol trifenatate selectively activates airway β₂ adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol trifenatate can be used in asthma research^[2][4]. 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 trifenatate (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^[4].

Vilanterol trifenatate (5 μM, 30 min) undergoes rapid metabolic inactivation in the systemic circulation during human liver microsome experiments^[4].

Vilanterol trifenatate has moderate membrane permeability in MDCKII-MDR1 cells (P_app = 34 nm/s), which may reduce systemic absorption^[4].

Vilanterol trifenatate is highly selective for β₂-AR, with at least 1000-fold selectivity for the β₂-AR and β₃-AR subtypes^[2].

In Vivo:Vilanterol trifenatate (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^[4].