Vilanterol-d₄ trifenatate  (Synonyms: GW642444-d₄ trifenatate)

Vilanterol-d₄ (trifenatate) is deuterium labeled Vilanterol (trifenatate).Vilanterol (GW642444) acetate is a long-acting β₂ adrenergic receptor agonist. Vilanterol acetate has pEC₅₀ values for β₂-AR, β₁-AR, and β₃-AR of 9.4, 6.4, and 6.1, respectively. Vilanterol acetate selectively activates airway β₂ adrenergic receptors, increases cAMP and thus relaxes bronchial smooth muscle. Vilanterol acetate can be used in asthma research.

Stable heavy isotopes of hydrogen, carbon, and other elements have been incorporated into drug molecules, largely as tracers for quantitation during the drug development process. Deuteration has gained attention because of its potential to affect the pharmacokinetic and metabolic profiles of drugs^[1].

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

778.79

C₄₄H₄₅D₄Cl₂NO₇

2021249-10-3

503070-58-4

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216.  [Content Brief]

  [2]. 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]

  [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]