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。