Vilanterol trifenatate|GW642444M|DC Chemcials
Vilanterol trifenatate (GW642444)is a novel, inhaled, long-acting β(2) agonist with inherent 24-h activity under development as a once-daily combination therapy with an inhaled corticosteroid for COPD and asthma.
Product Name: Vilanterol trifenatate |Catalog Number: DC8480 |CAS 503070-58-4 |Other names: GW642444M; GW 642444M; GW-642444M |Chemical Name: |Molecule Formular: C44H49Cl2NO7 |MW: 774.77
Vilanterol trifenatate (GW642444)is a novel, inhaled, long-acting β(2) agonist with inherent 24-h activity under development as a once-daily combination therapy with an inhaled corticosteroid for COPD and asthma.
in vitro: 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. Vilanterolalso showed a level of intrinsic efficacy that was comparable to indacaterol but significantly greater than that of salmeterol.
in vivo: The combination of FF/VI at a strength of 100/25 μg significantly (p < 0.001) improved wm FEV1 (173 ml) and trough FEV1 (115 ml) vs. placebo. Similar effects were observed with FF/VI 50/25 μg. VI 25 μg over 24 weeks improved lung function vs. placebo significantly for wm FEV1 (103 ml, p < 0.001) and trough FEV1 (67 ml, p = 0.017).
Toxicity: All doses of VI were associated with a low incidence of treatment-related adverse events/serious adverse events, with no suggestion of effects on BP, pulse rate, QT intervals corrected for heart rate calculated by Fridericia formula, or blood glucose and potassium levels.
For research and scientific purpose only, not for human use.
没有评论:
发表评论