化学信息：
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化学名
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4-[(1R)-2-[6-[2-[(2,6-dichlorophenyl)methoxy]ethoxy]hexylamino]-1-hydroxyethyl]-2-(hydroxymethyl)phenol
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简称
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Vilanterol
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别名
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GW 642444X, GW 642444, GW642444X, GW642444, GW-642444X, GW-642444
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中文名
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维兰特罗
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化学式
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C24H33Cl2NO5
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分子量
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486.43
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CAS号
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503068-34-6
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纯度
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98%
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溶剂/溶解度
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Water<1mg/ml; DMSO5mg/ml; Ethanol<1mg/ml
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溶液配制
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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。
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生物信息：
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产品描述
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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.
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信号通路
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GPCR & G Protein
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靶点
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β2 agonist
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－
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－
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－
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－
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IC50
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－
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－
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－
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－
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－
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体外研究
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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.
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体内研究
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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).
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临床实验
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N/A
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特征
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N/A
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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)：
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酶活性检测实验
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方法
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N/A
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细胞实验
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细胞系
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N/A
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浓度
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N/A
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处理时间
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N/A
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方法
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N/A
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动物实验
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动物模型
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N/A
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配制
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N/A
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剂量
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N/A
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给药方式
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N/A
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参考文献：
1. Slack RJ, et al. J Pharmacol Exp Ther. 2013 Jan, 344(1), 218-30.
2. Slack RJ, et al. J Pharmacol Exp Ther. 2013 Jan, 344(1), 218-30.
3. Kerwin EM, et al. Respir Med. 2013 Apr, 107(4), 560-9.
4. Hanania NA, et al. Chest. 2012 Jul, 142(1), 119-27.
包装清单：
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产品编号
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产品名称
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包装
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SD2443-10mM
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Vilanterol (β2激动剂)
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10mM×0.2ml
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SD2443-5mg
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Vilanterol (β2激动剂)
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5mg
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SD2443-25mg
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Vilanterol (β2激动剂)
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25mg
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—
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说明书
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1份
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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。
注意事项：
本产品仅限于专业人员的科学研究用，不得用于临床诊断或治疗，不得用于食品或药品，不得存放于普通住宅内。
为了您的安全和健康，请穿实验服并戴一次性手套操作。
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