Vilanterol (β2激动剂)

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。

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

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IC50

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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

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

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说明书

1份