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Vilanterol trifenatate

CAS No. : 503070-58-4

MCE 站：Vilanterol trifenatate

产品活性：Vilanterol trifenatate (GW642444 trifenatate) 是一种长效的 β₂-AR 激动剂，效力持续24小时。 对β₂-AR，β₁-AR和β₃-AR的 pEC₅₀ 分别为10.37，6.98 ，7.36。

研究领域：GPCR/G Protein  |  Neuronal Signaling

作用靶点：Adrenergic Receptor

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. 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. 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.

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