Vilanterol trifenatate 是一种长效的β2-AR激动剂，效力持续24小时，能够作用于β2-AR (pEC50=10.37)，β1-AR (pEC50=6.98) 和 β3-AR (pEC50=7.36)。

Vilanterol trifenatate is a long-acting agonist of β2-adrenoceptor (β2-AR) with inherent 24-hour activity(β2-AR, β1-AR and β3-AR pEC50s of 10.37, 6.98 and 7.36, respectively)

The preclinical pharmacological profile of vilanterol using radioligand binding and cAMP studies in recombinant assays as well as human and guinea pig tissue systems to characterize β(2)-AR binding and functional properties.?Vilanterol displayed a subnanomolar affinity for the β(2)-AR that was comparable with that of salmeterol but higher than olodaterol, formoterol, and indacaterol.?In cAMP functional activity studies, vilanterol demonstrated similar selectivity as salmeterol for β(2)- over β(1)-AR and β(3)-AR, but a significantly improved selectivity profile than formoterol and indacaterol.?Vilanterol also showed a level of intrinsic efficacy that was comparable to indacaterol but significantly greater than that of salmeterol.

503070-58-4

C44H49Cl2NO7

774.78

维兰特罗三苯乙酸盐;GW642444 (trifenatate);Vilanterol trifenatate

DMSO:100 mg/mL (129.07 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years