Vilanterol trifenatate
Based on 6 publication(s) in Google Scholar
Vilanterol (GW642444) trifenatate is a long-acting β2 adrenergic receptor agonist. Vilanterol trifenatate has pEC50 values for β2-AR, β1-AR, and β3-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol trifenatate selectively activates airway β2 adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol trifenatate can be used in asthma research[2][4].
연구목적의 판매만을 진행합니다. 환자를 대상으로 한 판매는 하지 않습니다.
- Purity : 99.82%
- CAS No.: 503070-58-4
- 화학식: C44H49Cl2NO7
- 분자량:774.77
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보관:
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Vilanterol trifenatate
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Customer Validation & Images
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WB
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WB
All Adrenergic Receptor Isoforms
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Biological Activity
제품 설명
IC50 & Target
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β adrenergic receptor |
In Vitro
Vilanterol trifenatate (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[4].
Vilanterol trifenatate (5 μM, 30 min) undergoes rapid metabolic inactivation in the systemic circulation during human liver microsome experiments[4].
Vilanterol trifenatate has moderate membrane permeability in MDCKII-MDR1 cells (P_app = 34 nm/s), which may reduce systemic absorption[4].
Vilanterol trifenatate 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. .
In Vivo
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[4]
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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.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
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| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 503070-58-4
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Appearance Solid
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분자량 774.77
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화학식 C44H49Cl2NO7
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Color White to off-white
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SMILES
OC1=CC=C([C@@H](O)CNCCCCCCOCCOCC2=C(Cl)C=CC=C2Cl)C=C1CO.O=C(O)C(C3=CC=CC=C3)(C4=CC=CC=C4)C5=CC=CC=C5
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Synonyms
GW642444 trifenatate
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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 trifenatate 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 trifenatate 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.
용액&용해도
In Vitro:
DMSO : 50 mg/mL (64.54 mM; ultrasonic and warming and heat to 60°C; 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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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 mg/mL (2.58 mM); Clear solution; Need ultrasonic
This protocol yields a clear solution of 2 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 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 mg/mL (2.58 mM); Suspended solution; Need ultrasonic
This protocol yields a suspended solution of 2 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 (20.0 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.
In Vivo Dissolution Calculator
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
순도&문서
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Data Sheet (288 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Handling Instructions (2659 KB)
References
[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]. 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]. 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]
[4]. 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 (sealed storage, away from moisture). 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 |
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| DMSO | 1 mM | 1.2907 mL | 6.4535 mL | 12.9071 mL | 32.2676 mL |
| 5 mM | 0.2581 mL | 1.2907 mL | 2.5814 mL | 6.4535 mL | |
| 10 mM | 0.1291 mL | 0.6454 mL | 1.2907 mL | 3.2268 mL | |
| 15 mM | 0.0860 mL | 0.4302 mL | 0.8605 mL | 2.1512 mL | |
| 20 mM | 0.0645 mL | 0.3227 mL | 0.6454 mL | 1.6134 mL | |
| 25 mM | 0.0516 mL | 0.2581 mL | 0.5163 mL | 1.2907 mL | |
| 30 mM | 0.0430 mL | 0.2151 mL | 0.4302 mL | 1.0756 mL | |
| 40 mM | 0.0323 mL | 0.1613 mL | 0.3227 mL | 0.8067 mL | |
| 50 mM | 0.0258 mL | 0.1291 mL | 0.2581 mL | 0.6454 mL | |
| 60 mM | 0.0215 mL | 0.1076 mL | 0.2151 mL | 0.5378 mL |
Vilanterol trifenatate Related Classifications
HY-14300A Related Classifications
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