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Vilanterol Trifenate Adrenergic Receptor agonist

Name: Vilanterol Trifenate
Brand: Selleck Chemicals
SKU: S3727
Availability: InStock
Rating: 5 (3 reviews)

Cat.No.S3727

Vilanterol trifenatate (GW642444M) is a novel inhaled long-acting beta2 adrenoceptor agonist with inherent 24-hour activity for once daily treatment of COPD and asthma.

Chemical Structure

Molecular Weight: 774.77

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Quality Control

Batch: Purity: 99.73%

99.73

Related Targets	AChR 5-HT Receptor COX Calcium Channel Histamine Receptor Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Adrenergic Receptor Inhibitors	Zenidolol (ICI-118551) Hydrochloride Yohimbine HCl L755507 Atipamezole Higenamine hydrochloride Fenoterol hydrobromide Medetomidine HCl Rauwolscine hydrochloride Deoxycorticosterone acetate Detomidine HCl

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (129.07 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 14 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	7.500mg/ml (9.68mM)	Taking the 1 mL working solution as an example, add 50 μL of 150 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	0.500mg/ml (0.65mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

% Tween 80

% ddH₂O

% DMSO

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	774.77	Formula	C₂₄H₃₃Cl₂NO₅.C₂₀H₁₆O₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	503070-58-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	GW642444M Trifenate			Smiles	OCC1=CC(=CC=C1O)C(O)CNCCCCCCOCCOCC2=C(Cl)C=CC=C2Cl.OC(=O)C(C3=CC=CC=C3)(C4=CC=CC=C4)C5=CC=CC=C5

Mechanism of Action

Targets/IC₅₀/Ki	β2-adrenoceptor
In vitro	Vilanterol displays a subnanomolar affinity for the β2-AR that is comparable with that of salmeterol but higher than olodaterol, formoterol, and indacaterol. In cAMP functional activity studies, vilanterol demonstrates similar selectivity as salmeterol for β2- over β1-AR and β3-AR, but a significantly improved selectivity profile than formoterol and indacaterol. Vilanterol also shows a level of intrinsic efficacy that is comparable to indacaterol but significantly greater than that of salmeterol. In cellular cAMP production and tissue-based studies measuring persistence and reassertion, vilanterol has a persistence of action comparable with indacaterol and longer than formoterol. In addition, vilanterol demonstrates reassertion activity in both cell and tissue systems that is comparable with salmeterol and indacaterol but longer than formoterol. In human airways, vilanterol is shown to have a faster onset and longer duration of action than salmeterol, exhibiting a significant level of bronchodilation 22 h after treatment.
References	[1] https://pubmed.ncbi.nlm.nih.gov/23131596/

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