Vilanterol (Synonyms: 维兰特罗; GW642444)

目录号: HY-14300 纯度: 99.30%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

Vilanterol (GW642444) 是一种长效的 β₂-AR 激动剂，效力持续24小时。对β₂-AR，β₁-AR和β₃-AR的 pEC₅₀ 分别为10.37，6.98 ，7.36。

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Vilanterol Chemical Structure

CAS No. : 503068-34-6

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5 mg	￥900	In-stock
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100 mg	￥5720	In-stock
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Customer Review

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Vilanterol trifenatate In-stock

MCE 顾客使用本产品发表的 5 篇科研文献

: Vilanterol purchased from MCE. Usage Cited in: Centre for Neuroscience. University of Alberta. 2016.; β-arrestin2 is important in the β2-AR agonist-mediated inhibition of TNF-β, but not in β2-AR agonist-mediated IL-10 enhancement. Western blot showing silencing β-arrestin2 expression.

: Vilanterol purchased from MCE. Usage Cited in: Mental Health and Neuroscience Institute. University of Alberta. 2016 Sep.; The objective of the next set of experiments is to determine if the (i) super long-acting 2-AR agonists Indacaterol and Vilanterol inhibit TNF-α in a β-arrestin2-dependent manner, and (ii) whether β-arrestin2 is involved in the anti-inflammatory conversion leading to the up-regulation of IL-10 production by these β2-AR agonists.

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α adrenergic receptor β adrenergic receptor

生物活性
实验参考方法
纯度 & 产品资料
参考文献

生物活性

Vilanterol (GW642444) is a long-acting β₂-adrenoceptor (β₂-AR) agonist with 24 h activity. The pEC₅₀s for β₂-AR,β₁-AR and β₃-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.

IC₅₀ & Target

β adrenergic receptor

体外研究
(In Vitro)

The selectivity of Vilanterol for β₂-AR over the other β-AR receptor subtypes (β₂ and β₃) is established by testing the ability of Vilanterol to elicit concentration-dependent increases in cAMP in CHO cells expressing human β₁-, β₂-, and β₃-AR. Vilanterol is demonstrated to be highly selective for the β₂-AR with at least a 1000-fold selectivity over both β₂- and β₃-AR subtypes. This analysis results in a low-affinity pK_D for [³H]Vilanterol of 9.44±0.07 (n=4) in the presence Gpp(NH)p and a high-affinity pK_D of 10.82±0.12 (n=4) and a low-affinity pK_D 9.47±0.17 (n=4) in the absence of Gpp(NH)p. In addition, a low-affinity pK_D for [³H]Vilanterol of 9.52±0.24 (n=4) in the absence of Gpp(NH)p (37°C) is observed^[1]. Vilanterol trifenatate is a novel inhaled long-acting β₂-agonist with inherent 24 h activity in vitro in development as a combination with the inhaled corticosteroid fluticasone furoate for both COPD and asthma^[2]. Vilanterol is a novel long-acting β₂-agonist (LABA) with inherent 24-hour activity for once-daily clinical treatment of chronic obstructive pulmonary disease (COPD) and asthma in combination with the inhaled novel corticosteroid fluticasone furoate, also active for 24 hours^[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

486.43

Formula

C₂₄H₃₃Cl₂NO₅

CAS 号

503068-34-6

性状

油状物

颜色

Light yellow to yellow

中文名称

维兰特罗

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。

以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：
——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；
以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

方案一

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.14 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水定容至 1 mL。
生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
方案二

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.14 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
20% SBE-β-CD in Saline 的配制（4°C，储存一周）：2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。
方案三

请依序添加每种溶剂： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.14 mM); 澄清溶液

此方案可获得 ≥ 2.5 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

计算结果

工作液所需浓度 : mg/mL

纯度 & 产品资料

纯度: 99.30%

选择批次：

Data Sheet (562 KB) SDS (252 KB)

COA (187 KB) HNMR (471 KB) LCMS (90 KB)

产品使用指南 (1538 KB)

参考文献

[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 [Content Brief]

[2]. Calzetta L, et al. Pharmacological characterization of the interaction between umeclidinium and vilanterol in human bronchi. Eur J Pharmacol. 2017 Jul 14. pii: S0014-2999(17)30470-3. [Content Brief]

[3]. 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- [Content Brief]

[4]. Harrell AW, et al. Metabolism and disposition of Vilanterol, a long-acting β(2)-adrenoceptor agonist for inhalation use in humans. Drug Metab Dispos. 2013 Jan;41(1):89-100. [Content Brief]

Kinase Assay ^[1]	Saturation, association, and dissociation binding studies are performed for [³H]Vilanterol to determine receptor binding kinetics at the β₂-AR (equilibrium dissociation constant (K_D), total number of receptors (Bmax), association rate (k_on), and dissociation rate (k_off) are calculated). For saturation binding, membranes (in a volume of 1.4 mL to avoid ligand depletion) are incubated with increasing concentrations of [³H]Vilanterol (~0.01-1.3 nM) for 5 h before filtration. For association binding, membranes are incubated with different concentrations of [³H]Vilanterol (~0.1-1.9 nM) for varying incubation times up to 1 h before filtration. For dissociation binding, membranes are preincubated for 1 h with a fixed concentration of [³H]Vilanterol (~1.1 nM) before dissociation is initiated by a 1:20 dilution in binding buffer (containing 10 μM cold Vilanterol) and then incubated for varying times up to 8 h before filtration. Saturation binding is also completed for [³H]CGP12177 (increasing concentrations of ~0.01-2.8 nM) in the same format as described above for [³H]Vilanterol. To determine the affinity of β₂-AR agonists and antagonists, competition binding displacement studies are completed in which membranes are incubated with a fixed concentration of [³H]Vilanterol (~0.2 nM) and increasing concentrations of unlabeled agonist/antagonist for 5 h before filtration. All competition binding displacement studies are completed in the presence of 100 µM Gpp(NH)p to ensure that binding curves are monophasic^[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
参考文献	[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 [Content Brief] [2]. Calzetta L, et al. Pharmacological characterization of the interaction between umeclidinium and vilanterol in human bronchi. Eur J Pharmacol. 2017 Jul 14. pii: S0014-2999(17)30470-3. [Content Brief] [3]. 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- [Content Brief] [4]. Harrell AW, et al. Metabolism and disposition of Vilanterol, a long-acting β(2)-adrenoceptor agonist for inhalation use in humans. Drug Metab Dispos. 2013 Jan;41(1):89-100. [Content Brief]

Kinase Assay
^[1]

Saturation, association, and dissociation binding studies are performed for [³H]Vilanterol to determine receptor binding kinetics at the β₂-AR (equilibrium dissociation constant (K_D), total number of receptors (Bmax), association rate (k_on), and dissociation rate (k_off) are calculated). For saturation binding, membranes (in a volume of 1.4 mL to avoid ligand depletion) are incubated with increasing concentrations of [³H]Vilanterol (~0.01-1.3 nM) for 5 h before filtration. For association binding, membranes are incubated with different concentrations of [³H]Vilanterol (~0.1-1.9 nM) for varying incubation times up to 1 h before filtration. For dissociation binding, membranes are preincubated for 1 h with a fixed concentration of [³H]Vilanterol (~1.1 nM) before dissociation is initiated by a 1:20 dilution in binding buffer (containing 10 μM cold Vilanterol) and then incubated for varying times up to 8 h before filtration. Saturation binding is also completed for [³H]CGP12177 (increasing concentrations of ~0.01-2.8 nM) in the same format as described above for [³H]Vilanterol. To determine the affinity of β₂-AR agonists and antagonists, competition binding displacement studies are completed in which membranes are incubated with a fixed concentration of [³H]Vilanterol (~0.2 nM) and increasing concentrations of unlabeled agonist/antagonist for 5 h before filtration. All competition binding displacement studies are completed in the presence of 100 µM Gpp(NH)p to ensure that binding curves are monophasic^[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献

[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 [Content Brief]

[2]. Calzetta L, et al. Pharmacological characterization of the interaction between umeclidinium and vilanterol in human bronchi. Eur J Pharmacol. 2017 Jul 14. pii: S0014-2999(17)30470-3. [Content Brief]

[3]. 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- [Content Brief]

[4]. Harrell AW, et al. Metabolism and disposition of Vilanterol, a long-acting β(2)-adrenoceptor agonist for inhalation use in humans. Drug Metab Dispos. 2013 Jan;41(1):89-100. [Content Brief]

Vilanterol 相关分类

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Vilanterol (Synonyms: 维兰特罗; GW642444)

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MCE 顾客使用本产品发表的 5 篇科研文献

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•同靶点产品:

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查看 Adrenergic Receptor 亚型特异性产品:

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参考文献

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Vilanterol (Synonyms: 维兰特罗; GW642444)

Customer Review

Other Forms of Vilanterol:

Vilanterol 相关抗体

MCE 顾客使用本产品发表的 5 篇科研文献

Vilanterol 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Adrenergic Receptor 亚型特异性产品:

生物活性

实验参考方法

纯度 & 产品资料

参考文献

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