2. GPCR/G Protein Neuronal Signaling
  3. Adrenergic Receptor
  4. Vilanterol acetate

Vilanterol acetate  (Synonyms: GW642444 acetate)

目录号: HY-14300D
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Vilanterol (GW642444) acetate 是一种长效 β2-AR 激动剂。Vilanterol acetate 对 β2-AR，β1-AR 和 β3-AR 的 pEC50 分别为 9.4，6.4，6.1。Vilanterol acetate 选择性激活气道 β2-AR 受体，升高 cAMP 从而舒张支气管平滑肌。Vilanterol acetate 可用于哮喘的相关研究[1][2]。

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Vilanterol acetate

Vilanterol acetate Chemical Structure

CAS No. : 503068-35-7

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Vilanterol acetate 的其他形式现货产品:

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Vilanterol acetate 相关抗体

Top Publications Citing Use of Products

    Vilanterol acetate purchased from MCE. Usage Cited in: 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 acetate 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

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Vilanterol (GW642444) acetate is a long-acting β2 adrenergic receptor agonist. Vilanterol acetate has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research[1][2].

    体外研究
    (In Vitro)

    Vilanterol acetate (Compound 13f) 是一种在转染了人 β1、β2 和 β3 受体的中国仓鼠卵巢细胞 (CHO) 中高效 (β2: pEC50 = 9.4)、高活性 (IA = 0.69) 且高选择性 (pEC50 差异: β2/β1 = 3.0) 的 β2 受体激动剂[1]。

    Vilanterol acetate (5 μM, 30 min) 在人肝微粒体实验中，在全身循环中快速代谢失活[1]。

    Vilanterol acetate 在 MDCKII-MDR1 细胞中膜渗透性中等 (P_app = 34 nm/s)，可能减少全身吸收[1]。

    Vilanterol acetate 对 β2-AR 具有高度选择性，其对 β2-AR和 β3-AR 亚型的选择性至少高出 1000 倍[2]。

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

    Vilanterol acetate 相关抗体:
    体内研究
    (In Vivo)

    Vilanterol acetate (Compound 13f) (30 μM, 300 μM, 雾化吸入, 单次给药) 对吸入后体内支气管扩张具有持久作用，给药剂量越高，这种作用的持续时间越长，可以显著缓解组胺诱导的豚鼠支气管痉挛中的哮喘症状[1]。

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

    Animal Model: Histamine-induced bronchospasm in the guinea pig model[1]
    Dosage: EC90 = 30 μM, 300 μM
    Administration: Nebulizer inhalation (Neb. Inh.), once dose.
    Result: Exhibited a duration of action of 10 hours at an EC90 of 30 μM and 17 hours at an EC90 of 300 μM.
    分子量

    546.48

    Formula

    C26H37Cl2NO7
    CAS 号
    运输条件

    Room temperature in continental US; may vary elsewhere.
    储存方式

    Please store the product under the recommended conditions in the Certificate of Analysis.
    纯度 & 产品资料
    参考文献

    Vilanterol acetate 相关分类

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    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Vilanterol503068-35-7GW642444GW 642444GW-642444Adrenergic ReceptorBeta ReceptorCHO cellsMDCKII-MDR1 cellsguinea pigAsthmaChronic Obstructive Pulmonary Disease (COPD)Inhibitorinhibitorinhibit

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