tcsc1679 Vilanterol (trifenatate)

Vilanterol trifenatate is a long-acting β₂-adrenoceptor (β₂-AR) agonist with 24 h activity. The pEC₅₀s for β₂-AR,β₁-AR and β₃-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.

IC50 & Target: pEC50: 10.37±0.05 (β₂-adrenoceptor), 6.98±0.03 (β₁-adrenoceptor), 7.36±0.03 (β₃-adrenoceptor)^[1]

In Vitro: The selectivity of Vilanterol trifenatate for β₂-AR over the other β-AR receptor subtypes (β₂ and β₃) is established by testing the ability of Vilanterol to elicit concentration-dependent increases in cAMP in CHO cells expressing human β₁-, β₂-, and β₃-AR. Vilanterol is demonstrated to be highly selective for the β₂-AR with at least a 1000-fold selectivity over both β₂- and β₃-AR subtypes. This analysis results in a low-affinity pK_D for [³H]Vilanterol of 9.44±0.07 (n=4) in the presence Gpp(NH)p and a high-affinity pK_D of 10.82±0.12 (n=4) and a low-affinity pK_D 9.47±0.17 (n=4) in the absence of Gpp(NH)p. In addition, a low-affinity pK_D for [³H]Vilanterol of 9.52±0.24 (n=4) in the absence of Gpp(NH)p (37°C) is observed^[1]. Vilanterol trifenatate is a novel inhaled long-acting β₂-agonist with inherent 24 h activity in vitro in development as a combination with the inhaled corticosteroid fluticasone furoate for both COPD and asthma^[2]. Vilanterol is a novel long-acting β₂-agonist (LABA) with inherent 24-hour activity for once-daily clinical treatment of chronic obstructive pulmonary disease (COPD) and asthma in combination with the inhaled novel corticosteroid fluticasone furoate, also active for 24 hours^[3].