Vilanterol (Synonyms: GW642444)

Name: Vilanterol
Brand: MedChemExpress
SKU: HY-14300
Rating: 5.0 (7 reviews)

Cat. No.: HY-14300 Purity: 99.30%: FAQs
Data Sheet SDS COA Handling Instructions

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Vilanterol (GW642444) is a long-acting β₂-adrenoceptor (β₂-AR) agonist with 24 h activity. The pEC₅₀s for β₂-AR,β₁-AR and β₃-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.

For research use only. We do not sell to patients.

Vilanterol Chemical Structure

CAS No. : 503068-34-6

Size	Price	Stock	Quantity
Oil + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 118	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 118	In-stock	Estimated Time of Arrival: December 31
Oil
1 mg	USD 52	In-stock	Estimated Time of Arrival: December 31
5 mg	USD 110	In-stock	Estimated Time of Arrival: December 31
10 mg	USD 165	In-stock	Estimated Time of Arrival: December 31
50 mg	USD 495	In-stock	Estimated Time of Arrival: December 31
100 mg	USD 715	In-stock	Estimated Time of Arrival: December 31
200 mg		Get quote
500 mg		Get quote

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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Vilanterol:

Vilanterol trifenatate In-stock

5 Publications Citing Use of MCE Vilanterol

: Vilanterol purchased from MedChemExpress. Usage Cited in: Centre for Neuroscience. 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 purchased from MedChemExpress. 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

Biological Activity
Protocol
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

β adrenergic receptor

In Vitro

The selectivity of Vilanterol for β₂-AR over the other β-AR receptor subtypes (β₂ and β₃) is established by testing the ability of Vilanterol to elicit concentration-dependent increases in cAMP in CHO cells expressing human β₁-, β₂-, and β₃-AR. Vilanterol is demonstrated to be highly selective for the β₂-AR with at least a 1000-fold selectivity over both β₂- and β₃-AR subtypes. This analysis results in a low-affinity pK_D for [³H]Vilanterol of 9.44±0.07 (n=4) in the presence Gpp(NH)p and a high-affinity pK_D of 10.82±0.12 (n=4) and a low-affinity pK_D 9.47±0.17 (n=4) in the absence of Gpp(NH)p. In addition, a low-affinity pK_D for [³H]Vilanterol of 9.52±0.24 (n=4) in the absence of Gpp(NH)p (37°C) is observed^[1]. Vilanterol trifenatate is a novel inhaled long-acting β₂-agonist with inherent 24 h activity in vitro in development as a combination with the inhaled corticosteroid fluticasone furoate for both COPD and asthma^[2]. Vilanterol is a novel long-acting β₂-agonist (LABA) with inherent 24-hour activity for once-daily clinical treatment of chronic obstructive pulmonary disease (COPD) and asthma in combination with the inhaled novel corticosteroid fluticasone furoate, also active for 24 hours^[3].

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

Clinical Trial

Molecular Weight

486.43

Formula

C₂₄H₃₃Cl₂NO₅

CAS No.

503068-34-6

Appearance

Oil

Color

Light yellow to yellow

SMILES

OC1=CC=C([C@@H](O)CNCCCCCCOCCOCC2=C(Cl)C=CC=C2Cl)C=C1CO

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Pure form	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.0558 mL	10.2790 mL	20.5579 mL
5 mM	0.4112 mL	2.0558 mL	4.1116 mL
10 mM	0.2056 mL	1.0279 mL	2.0558 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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator
Dilution Calculator

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: ≥ 2.5 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.
Protocol 2

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.14 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). 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 (25.0 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).

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.

Purity & Documentation

Purity: 99.30%

Select Batch:

Data Sheet (276 KB) SDS (252 KB)

COA (243 KB) HNMR (472 KB) LCMS (96 KB)

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]. 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]

Kinase Assay
^[1]

Saturation, association, and dissociation binding studies are performed for [³H]Vilanterol to determine receptor binding kinetics at the β₂-AR (equilibrium dissociation constant (K_D), total number of receptors (Bmax), association rate (k_on), and dissociation rate (k_off) are calculated). For saturation binding, membranes (in a volume of 1.4 mL to avoid ligand depletion) are incubated with increasing concentrations of [³H]Vilanterol (~0.01-1.3 nM) for 5 h before filtration. For association binding, membranes are incubated with different concentrations of [³H]Vilanterol (~0.1-1.9 nM) for varying incubation times up to 1 h before filtration. For dissociation binding, membranes are preincubated for 1 h with a fixed concentration of [³H]Vilanterol (~1.1 nM) before dissociation is initiated by a 1:20 dilution in binding buffer (containing 10 μM cold Vilanterol) and then incubated for varying times up to 8 h before filtration. Saturation binding is also completed for [³H]CGP12177 (increasing concentrations of ~0.01-2.8 nM) in the same format as described above for [³H]Vilanterol. To determine the affinity of β₂-AR agonists and antagonists, competition binding displacement studies are completed in which membranes are incubated with a fixed concentration of [³H]Vilanterol (~0.2 nM) and increasing concentrations of unlabeled agonist/antagonist for 5 h before filtration. All competition binding displacement studies are completed in the presence of 100 µM Gpp(NH)p to ensure that binding curves are monophasic^[1].

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

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]. 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]

Complete Stock Solution Preparation Table

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 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:

Vilanterol503068-34-6GW642444GW 642444GW-642444Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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Vilanterol (Synonyms: GW642444)

Customer Review

Other Forms of Vilanterol:

Vilanterol Related Antibodies

5 Publications Citing Use of MCE Vilanterol

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Adrenergic Receptor Isoform Specific Products:

Biological Activity

Protocol

Purity & Documentation

References

Customer Review

Vilanterol Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Vilanterol Related Classifications

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