| 生物活性: |
靶点:Adrenergic Receptor 通路:Endocrinology & Hormones;GPCR & G Protein;Neuronal Signaling 背景说明:是一种长效的 β2-AR 激动剂。 生物活性:Vilanterol Trifenate 是一种长效β2-肾上腺素受体(β2-AR)激动剂,具有 24 小时固有活性,对 β2-AR、β1-AR 和 β3-AR 的 pEC50 分别为 10.37、6.98 和 7.36。[1-2] In Vitro:Vilanterol trifenatate(vilanterol)displayed a subnanomolar affinity for the β(2)-AR,vilanterol demonstrated similar selectivity as salmeterol for β(2)- over β(1)-AR and β(3)-AR.[1] In Vivo:In human airways,vilanterol was shown to have a faster onset and longer duration of action than salmeterol,exhibiting a significant level of bronchodilation 22 h after treatment.[1] Vilanterol(VI; 25-100 μg; once daily,14 days)was well tolerated asthma and COPD,and produced a rapid and prolonged bronchodilation over 24 h.[2] 数据来源文献:[1]. Slack RJ,et al. In vitro pharmacological characterization of vilanterol,a novel long-acting β2-adrenoceptor agonist with 24-hour duration of action. J Pharmacol Exp Ther. 2013 Jan;344(1):218-30. [2]. Kempsford R,et al. Vilanterol trifenatate,a novel inhaled long-acting beta2 adrenoceptor agonist,is well tolerated in healthy subjects and demonstrates prolonged bronchodilation in subjects with asthma and COPD. Pulm Pharmacol Ther. 2013 Apr;26(2):256-64.
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| 其它标识: |
SMILES:C1=CC=C(C=C1)C(C2=CC=CC=C2)(C3=CC=CC=C3)C(=O)O.C1=CC(=C(C(=C1)Cl)COCCOCCCCCCNCC(C2=CC(=C(C=C2)O)CO)O)Cl InChIKey:KLOLZALDXGTNQE-JIDHJSLPSA-N InChI:InChI=1S/C24H33Cl2NO5.C20H16O2/c25-21-6-5-7-22(26)20(21)17-32-13-12-31-11-4-2-1-3-10-27-15-24(30)18-8-9-23(29)19(14-18)16-28;21-19(22)20(16-10-4-1-5-11-16,17-12-6-2-7-13-17)18-14-8-3-9-15-18/h5-9,14,24,27-30H,1-4,10-13,15-17H2;1-15H,(H,21,22)/t24-;/m0./s1 PubChem CID:44482554
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| 基本信息: |
CAS:503070-58-4 中文名称:维兰特罗三苯乙酸盐 英文名称:Vilanterol Trifenate 别名:GW642444M Trifenate 分子式:C44H49Cl2NO7 分子量:774.77 规格:1mg 溶解性:Soluble in DMSO ≥10mg/mL 纯度:≥98% 外观(性状):White to off-white Solid 储存条件:Powder:2-8℃,2 years;Insolvent(母液):-20℃,6 months;-80℃,1 year
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| 靶点: |
Adrenergic Receptor |