Vilanterol acetate
Based on 6 publication(s) in Google Scholar
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].
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- CAS 番号: 503068-35-7
- 分子式: C26H37Cl2NO7
- 分子量:546.48
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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生物活性
Vilanterol acetate (Compound 13f) is a highly efficient (β2: pEC50 = 9.4), highly active (IA = 0.69), and highly selective (pEC50 difference: β2/β1 = 3.0) β₂ receptor agonist in CHO cells transfected with human β1, β2, and β3 receptors[1].
Vilanterol acetate (5 μM, 30 min) undergoes rapid metabolic inactivation in the systemic circulation during human liver microsome experiments[1].
Vilanterol acetate has moderate membrane permeability in MDCKII-MDR1 cells (P_app = 34 nm/s), which may reduce systemic absorption[1].
Vilanterol acetate is highly selective for β2-AR, with at least 1000-fold selectivity for the β2-AR and β3-AR subtypes[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | CLplasma | Cmax |
|---|---|---|---|---|
| Rat | 0.25 mg/kg | i.v. | 123 mL/min/kg | / |
| Rat | 2 mg/kg | p.o. | / | <2 ng/mL |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Histamine-induced bronchospasm in the guinea pig model[1]
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Dosage:EC90 = 30 μM, 300 μM
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Administration:Nebulizer inhalation (Neb. Inh.), once dose.
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Result:Exhibited a duration of action of 10 hours at an EC90 of 30 μM and 17 hours at an EC90 of 300 μM.
化学情報
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CAS 番号 503068-35-7
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分子量 546.48
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分子式 C26H37Cl2NO7
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SMILES
OC1=CC=C([C@@H](O)CNCCCCCCOCCOCC2=C(Cl)C=CC=C2Cl)C=C1CO.CC(O)=O
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別名
GW642444 acetate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (6)
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Journal Impact Factor
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Most Recent
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Eur J Pharmacol
Pharmacological characterization of the interaction between umeclidinium and vilanterol in human bronchi. [Abstract]2017 Oct 5:812:147-154. PMID: 28716723 -
J Pharm Biomed Anal
Screening method of mildronate and over 300 doping agents by reversed-phase liquid chromatography-high resolution mass spectrometry. [Abstract]2021 Feb 20:195:113870. PMID: 33453569 -
Drug Test Anal
Supramolecular Solvent Extraction for Doping Control Analysis of Prohibited Substances in Horse Urine. [Abstract]2026 May;18(5):652-668. PMID: 41814125 -
J Neuroimmunol
Mechanism underlying β2-AR agonist-mediated phenotypic conversion of LPS-activated microglial cells. [Abstract]2019 Jul 15:332:37-48. PMID: 30933849 -
Vilanterol acetate purchased from MedChemExpress. 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.
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Vilanterol acetate purchased from MedChemExpress. Usage Cited in: 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.
純度とドキュメンテーション
参考文献
[1]. Panayiotis A Procopiou, et al. Synthesis and structure-activity relationships of long-acting beta2 adrenergic receptor agonists incorporating metabolic inactivation: an antedrug approach. J Med Chem. 2010 Jun 10. 53(11):4522-30. [Content Brief]
[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- [Content Brief]
[3]. 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]
Calculators
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Vilanterol acetate 関連分類
HY-14300D 関連分類
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