Vilanterol-d₁₂  (Synonyms: GW642444-d₁₂)

Vilanterol-d₁₂ (GW642444-d₁₂) is deuterium labeled Vilanterol. 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.

氢、碳和其他元素的稳定重同位素已被掺入药物分子中，主要用作药物开发过程中定量的示踪剂。氘化因其可能影响药物的药代动力学和代谢特征而受到关注。

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

498.50

GW642444-d₁₂

C₂₄H₂₁D₁₂Cl₂NO₅

503068-34-6

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]. 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]

  [5]. 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]