化学信息：
| 化学名 | 4-[(1R)-2-[6-[2-[(2,6-dichlorophenyl)methoxy]ethoxy]hexylamino]-1-hydroxyethyl]-2-(hydroxymethyl)phenol |
|
| 简称 | Vilanterol | |
| 别名 |
GW 642444X, GW 642444, GW642444X, GW642444, GW-642444X, GW-642444 |
|
| 中文名 | 维兰特罗 | |
| 化学式 | C24H33Cl2NO5 | |
| 分子量 | 486.43 | |
| CAS号 | 503068-34-6 | |
| 纯度 | 98% | |
| 溶剂/溶解度 |
Water<1mg/ml; DMSO5mg/ml; Ethanol<1mg/ml |
|
| 溶液配制 | 5mg加入1.03ml DMSO，或者每4.86mg加入1ml DMSO，配制成10mM溶液。SD2443-10mM用DMSO配制。 |
生物信息：
| 产品描述 | Vilanterol (GW642444; GW 642444X) 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. | ||||
| 信号通路 | GPCR & G Protein | ||||
| 靶点 | β2 agonist | － | － | － | － |
| IC50 | － | － | － | － | － |
| 体外研究 | 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. | ||||
| 体内研究 | in vivo: The combination of FF/VI at a strength of 100/25μg significantly (p<0.001) improved wm FEV1 (173ml) and trough FEV1 (115ml) vs. placebo. Similar effects were observed with FF/VI 50/25μg. VI 25μg over 24weeks improved lung function vs. placebo significantly for wm FEV1 (103ml, p<0.001) and trough FEV1 (67ml, p=0.017). | ||||
| 临床实验 | N/A | ||||
| 特征 | N/A | ||||
相关实验数据(此数据来自于公开文献，碧云天并不保证其有效性)：
| 酶活性检测实验 | |
| 方法 | N/A |
| 细胞实验 | |
| 细胞系 | N/A |
| 浓度 | N/A |
| 处理时间 | N/A |
| 方法 | N/A |
| 动物实验 | |
| 动物模型 | N/A |
| 配制 | N/A |
| 剂量 | N/A |
| 给药方式 | N/A |
| 产品编号 | 产品名称 | 包装 |
| SD2443-10mM | Vilanterol (β2激动剂) | 10mM×0.2ml |
| SD2443-5mg | Vilanterol (β2激动剂) | 5mg |
| SD2443-25mg | Vilanterol (β2激动剂) | 25mg |
| — | 说明书 | 1份 |
保存条件：
-20℃保存，至少一年有效。5mg和25mg包装也可室温保存，至少6个月有效。如果溶于非DMSO溶剂，建议分装后-80℃保存，预计6个月内有效。
