Vilanterol acetate  (Synonyms: GW642444 acetate)

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^[1][2].

Vilanterol acetate (Compound 13f) is a highly efficient (β₂: pEC₅₀ = 9.4), highly active (IA = 0.69), and highly selective (pEC₅₀ difference: β₂/β₁ = 3.0) β₂ receptor agonist in CHO cells transfected with human β₁, β₂, and β₃ receptors^[1].

Vilanterol acetate (5 μM, 30 min) undergoes rapid metabolic inactivation in the systemic circulation during human liver microsome experiments^[1].

Vilanterol acetate has moderate membrane permeability in MDCKII-MDR1 cells (P_app = 34 nm/s), which may reduce systemic absorption^[1].

Vilanterol acetate is highly selective for β₂-AR, with at least 1000-fold selectivity for the β₂-AR and β₃-AR subtypes^[2].

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

Vilanterol acetate (Compound 13f) (30 μM, 300 μM, Nebulizer inhalation, Once dose) exerts a long-lasting effect on in vivo bronchial dilation following inhalation. The higher the administered dose, the longer the duration of this effect, and it can significantly alleviate asthma symptoms in histamine-induced bronchospasm in the guinea pig^[1].

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

546.48

C₂₆H₃₇Cl₂NO₇

503068-35-7

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

Room temperature in continental US; may vary elsewhere.

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

• [1]. 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.  [Content Brief]

  [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-  [Content Brief]

  [3]. 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]