Vilanterol trifenatate (Synonyms: GW642444 trifenatate)

Name: Vilanterol trifenatate
Brand: MedChemExpress
SKU: HY-14300A
Rating: 5.0 (6 reviews)

Cat. No.: HY-14300A Pureza: 99.82%: Ficha de datos
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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].

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No. CAS : 503070-58-4

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	En stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	En stock	Estimated Time of Arrival: December 31
Solid
5 mg	En stock	Estimated Time of Arrival: December 31
10 mg	En stock	Estimated Time of Arrival: December 31
25 mg	En stock	Estimated Time of Arrival: December 31
50 mg	En stock	Estimated Time of Arrival: December 31
100 mg	En stock	Estimated Time of Arrival: December 31
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Based on 6 publication(s) in Google Scholar

Other Forms of Vilanterol trifenatate:

Vilanterol In-stock
Vilanterol-d₄ trifenatate Obtener un presupuesto
Vilanterol acetate Obtener un presupuesto

6 Publications Citing Use of MCE Vilanterol trifenatate

: 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.

: 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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Ver todos los productos específicos de isoformas Adrenergic Receptor:

Ver todas las isoformas

α adrenergic receptor β adrenergic receptor

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Revisión del cliente

Descripciòn

IC₅₀ & Target

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

Vilanterol trifenatate (Compound 13f) (30 μM, 300 μM, Nebulizer inhalation, Once dose) exerts a long-lasting effect on in vivo bronchial dilation following inhalation. The higher the administered dose, the longer the duration of this effect, and it can significantly alleviate asthma symptoms in histamine-induced bronchospasm in the guinea pig^[4].

MedChemExpress (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^[4]
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.

Ensayo clínico

Peso molecular

774.77

Fòrmula

C₄₄H₄₉Cl₂NO₇

No. CAS

503070-58-4

Appearance

Solid

Color

White to off-white

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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvente y solubilidad

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	1.2907 mL	6.4535 mL	12.9071 mL
5 mM	0.2581 mL	1.2907 mL	2.5814 mL
10 mM	0.1291 mL	0.6454 mL	1.2907 mL

View the 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.

Calculadora de molaridad
Calculadora de dilución

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

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.

Protocol 1

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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: 2 mg/mL (2.58 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: 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)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

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.

Pureza y Documentación

Purity: 99.82%

Select Batch:

Ficha de datos (279 KB) SDS (393 KB)

COA (249 KB) HNMR (297 KB) LCMS (91 KB)

Instrucciones de manejo (2659 KB)

Referencias

[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

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

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

Help & FAQs

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:

Vilanterol503070-58-4GW642444GW 642444GW-642444Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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Vilanterol trifenatate (Synonyms: GW642444 trifenatate)

Revisión del cliente

Other Forms of Vilanterol trifenatate:

Vilanterol trifenatate Related Antibodies

6 Publications Citing Use of MCE Vilanterol trifenatate

Recomendaciones destacadas

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

Ver todos los productos específicos de isoformas Adrenergic Receptor:

Actividad biológica

Pureza y Documentación

Referencias

Revisión del cliente

Vilanterol trifenatate Related Antibodies

Calculadora de molaridad

Calculadora de dilución

Complete Stock Solution Preparation Table

Vilanterol trifenatate Related Classifications

Keywords:

Productos vistos recientemente:

Revisión del cliente

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