Vilanterol
Based on 6 publication(s) in Google Scholar
Vilanterol (GW642444) is a long-acting β2 adrenergic receptor agonist. Vilanterol has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol can be used in asthma research[3][5].
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 98.02%
- CAS 番号: 503068-34-6
- 分子式: C24H33Cl2NO5
- 分子量:486.43
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保管条件:Pure form -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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溶剤 & 溶解度
- 純度とドキュメンテーション
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MedChemExpress（MCE）の使用を引用している文献 Vilanterol
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Adrenergic Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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β adrenergic receptor |
Vilanterol (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[5].
Vilanterol (5 μM, 30 min) undergoes rapid metabolic inactivation in the systemic circulation during human liver microsome experiments[5].
Vilanterol has moderate membrane permeability in MDCKII-MDR1 cells (P_app = 34 nm/s), which may reduce systemic absorption[5].
Vilanterol is highly selective for β2-AR, with at least 1000-fold selectivity for the β2-AR and β3-AR subtypes[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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 503068-34-6
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性状 Oil
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分子量 486.43
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分子式 C24H33Cl2NO5
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Color Light yellow to yellow
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SMILES
OC1=CC=C([C@@H](O)CNCCCCCCOCCOCC2=C(Cl)C=CC=C2Cl)C=C1CO
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別名
GW642444
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Pure form -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
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 -
J Neuroimmunol
Mechanism underlying β2-AR agonist-mediated phenotypic conversion of LPS-activated microglial cells. [Abstract]2019 Jul 15:332:37-48. PMID: 30933849 -
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 -
Vilanterol 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 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.
溶剤 & 溶解度
DMSO : 100 mg/mL (205.58 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.14 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2.5 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
純度とドキュメンテーション
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データシート (275 KB)
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取扱説明書 (2659 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]
[5]. 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]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.0558 mL | 10.2790 mL | 20.5579 mL | 51.3949 mL |
| 5 mM | 0.4112 mL | 2.0558 mL | 4.1116 mL | 10.2790 mL | |
| 10 mM | 0.2056 mL | 1.0279 mL | 2.0558 mL | 5.1395 mL | |
| 15 mM | 0.1371 mL | 0.6853 mL | 1.3705 mL | 3.4263 mL | |
| 20 mM | 0.1028 mL | 0.5139 mL | 1.0279 mL | 2.5697 mL | |
| 25 mM | 0.0822 mL | 0.4112 mL | 0.8223 mL | 2.0558 mL | |
| 30 mM | 0.0685 mL | 0.3426 mL | 0.6853 mL | 1.7132 mL | |
| 40 mM | 0.0514 mL | 0.2570 mL | 0.5139 mL | 1.2849 mL | |
| 50 mM | 0.0411 mL | 0.2056 mL | 0.4112 mL | 1.0279 mL | |
| 60 mM | 0.0343 mL | 0.1713 mL | 0.3426 mL | 0.8566 mL | |
| 80 mM | 0.0257 mL | 0.1285 mL | 0.2570 mL | 0.6424 mL | |
| 100 mM | 0.0206 mL | 0.1028 mL | 0.2056 mL | 0.5139 mL |
Vilanterol 関連分類
HY-14300 関連分類
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