Vilanterol trifenatate

产品编号: DC8480 Featured
Vilanterol trifenatate
结构式
503070-58-4
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中国地区超过5000个高品质化合物库存
应用领域
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。
Cas No.: 503070-58-4
名称:
别名: GW642444M; GW 642444M; GW-642444M
SMILES: C(O)1=CC=C([C@H](O)CNCCCCCCOCCOCC2=C(Cl)C=CC=C2Cl)C=C1CO.C(O)(=O)C(C1=CC=CC=C1)(C1=CC=CC=C1)C1=CC=CC=C1
分子式: C44H49Cl2NO7
分子量: 774.77
纯度:
保存条件: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Description:
In Vivo:
In Vitro:
References: 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.
Kinase Assay:
Cell Assay:
Animal Administration:
References:
MSDS
COA
LOT NO. DOWNLOAD
2018-0101
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