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Vilanterol

SKU: orb1223111

Description

Vilanterol is a selective long-acting beta2-adrenergic agonist (LABA) used in the treatment of COPD and asthma.

Research Area

Pharmacology & Drug Discovery

Images & Validation

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Vilanterol

Key Properties

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CAS Number503068-34-6
MW486.43
Purity>98% (HPLC)
FormulaC24H33Cl2NO5
SMILESc1(c(cc(cc1)[C@H](CNCCCCCCOCCOCc1c(cccc1Cl)Cl)O)CO)O
Targetβ1-adrenoceptor| β2-adrenoceptor| β3-adrenoceptor
SolubilityDMSO : ≥ 100 mg/mL; 205.58 mM

Bioactivity

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In Vitro
The selectivity of Vilanterol for β2-AR over the other β-AR receptor subtypes (β2 and β3) is established by testing the ability of Vilanterol to elicit concentration-dependent increases in cAMP in CHO cells expressing human β1-, β2-, and β3-AR. Vilanterol is demonstrated to be highly selective for the β2-AR with at least a 1000-fold selectivity over both β2- and β3-AR subtypes. This analysis results in a low-affinity pKD for [3H]Vilanterol of 9.44±0.07 (n=4) in the presence Gpp(NH)p and a high-affinity pKD of 10.82±0.12 (n=4) and a low-affinity pKD 9.47±0.17 (n=4) in the absence of Gpp(NH)p. In addition, a low-affinity pKD for [3H]Vilanterol of 9.52±0.24 (n=4) in the absence of Gpp(NH)p (37°C) is observed. Vilanterol trifenatate is a novel inhaled long-acting β2-agonist with inherent 24 h activity in vitro in development as a combination with the inhaled corticosteroid fluticasone furoate for both COPD and asthma. Vilanterol is a novel long-acting β2-agonist (LABA) with inherent 24-hour activity for once-daily clinical treatment of chronic obstructive pulmonary disease (COPD) and asthma in combination with the inhaled novel corticosteroid fluticasone furoate, also active for 24 hours.

Storage & Handling

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StorageStorage temperature: -20°C. Stability: ≥ 2 years
Expiration Date12 months from date of receipt.
DisclaimerFor research use only

Alternative Names

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GW642444X | GW642444

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Quick Database Links

Gene Symbol
β1-adrenoceptor| β2-adrenoceptor| β3-adrenoceptor

Protocol Information

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