Vilanterol (trifenatate)

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].

Product Specifications

CAS Number

[503070-58-4]

Product Name Alternative

GW642444 (trifenatate)

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Adrenergic Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Endocrinology; Cancer

Assay Protocol

https://www.medchemexpress.com/Vilanterol-trifenatate.html

Purity

99.82

Solubility

DMSO : 50 mg/mL (ultrasonic; warming; heat to 60°C)

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

Molecular Formula

C44H49Cl2NO7

Molecular Weight

774.77

Precautions

H302, H315, H319, H335

References & Citations

[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|[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-|[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.|[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.

Shipping Conditions

Room Temperature

Storage Conditions

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Launched

Isoform

β adrenergic receptor

Citation 01

Mental Health and Neuroscience Institute. University of Alberta. 2016 Sep.|University of Alberta. 2016.|Eur J Pharmacol. 2017 Oct 5:812:147-154.|J Neuroimmunol. 2019 Jul 15:332:37-48.|J Pharm Biomed Anal. 2021 Feb 20:195:113870.