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| 25mg |
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Vilanterol (GW 642444; GW642444; GW-642444) is a long-acting β2-adrenoceptor/ beta-2 (β2-AR) agonist approved in May 2013 for use in combination with fluticasone furoate in the treatment of chronic obstructive pulmonary disease (COPD).
| Targets |
β adrenergic receptor
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|---|---|
| ln Vitro |
Vilanterol, in CHO cells expressing human β1-, β2-, and β3-AR, the ability of Vilanterol to elicit concentration-dependent increases in cAMP is used to determine selectivity for β2-AR over the other β-AR receptor subtypes (β2 and β3). Vilanterol is shown to have at least a 1000-fold selectivity over both β2- and β3-AR subtypes, indicating that it is highly selective for the β2-AR. Based on this analysis, the low-affinity pKD for [3H]Vilanterol in the presence of Gpp(NH)p is 9.44±0.07 (n=4), the high-affinity pKD is 10.82±0.12 (n=4), and the low-affinity pKD is 9.47±0.17 (n=4) in the absence of Gpp(NH)p. Furthermore, it is observed that at 37°C without Gpp(NH)p, a low-affinity pKD of 9.52±0.24 (n=4) for [3H]Vilanterol is present[1]. A new inhaled long-acting β2-agonist called vilanterol trifenatate is being developed as a combination with the inhaled corticosteroid fluticasone furoate to treat asthma and COPD. It has inherent 24-hour activity in vitro[2]. When used in conjunction with the inhaled novel corticosteroid fluticasone furoate, which is also active for 24 hours, vilanterol, a novel long-acting β2-agonist (LABA) with inherent 24-hour activity, can be used once daily for the clinical treatment of asthma and chronic obstructive pulmonary disease (COPD)[3].
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| Enzyme Assay |
For [3H]Vilanterol, binding kinetics studies involving saturation, association, and dissociation are carried out to calculate the equilibrium dissociation constant (KD), total number of receptors (Bmax), association rate (kon), and dissociation rate (koff). Membranes are filtered after being incubated with increasing concentrations of [3H]Vilanterol (0.01-1.3 nM) for 5 hours to achieve saturation binding (in a volume of 1.4 mL to prevent ligand depletion). Membranes are incubated with varying concentrations of [3H]Vilanterol (0.1-1.9 nM) for up to 1 hour prior to filtration in order to facilitate association binding. Membranes are preincubated with a fixed concentration of [3H]Vilanterol (1.1 nM) for 1 hour in order to facilitate dissociation binding. Dissociation is then triggered by dilution in binding buffer (10 μM cold Vilanterol), and incubation is continued for variable periods up to 8 hours prior to filtration. As with [3H]Vilanterol, saturation binding is also accomplished for [3H]CGP12177 (with concentrations rising to approximately 0.01-2.8 nM). Competition binding displacement studies, in which membranes are incubated with a fixed concentration of [3H]Vilanterol (0.2 nM) and increasing concentrations of unlabeled agonist/antagonist for 5 h before filtration, are carried out to ascertain the affinity of β2-AR agonists and antagonists. To guarantee that binding curves are monophasic, 100 µM Gpp(NH)p is present during the completion of all competition binding displacement studies[1].
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| References |
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| Molecular Formula |
C₂₄H₃₃CL₂NO₅
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|---|---|
| Molecular Weight |
486.43
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| Exact Mass |
485.17
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| Elemental Analysis |
C, 59.26; H, 6.84; Cl, 14.58; N, 2.88; O, 16.45
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| CAS # |
503068-34-6
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| Related CAS # |
Vilanterol trifenatate; 503070-58-4
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| Appearance |
A solution in ethanol
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| SMILES |
C1=CC(=C(C(=C1)Cl)COCCOCCCCCCNC[C@@H](C2=CC(=C(C=C2)O)CO)O)Cl
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| InChi Key |
DAFYYTQWSAWIGS-DEOSSOPVSA-N
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| InChi Code |
InChI=1S/C24H33Cl2NO5/c25-21-6-5-7-22(26)20(21)17-32-13-12-31-11-4-2-1-3-10-27-15-24(30)18-8-9-23(29)19(14-18)16-28/h5-9,14,24,27-30H,1-4,10-13,15-17H2/t24-/m0/s1
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| Chemical Name |
4-[(1R)-2-[6-[2-[(2,6-dichlorophenyl)methoxy]ethoxy]hexylamino]-1-hydroxyethyl]-2-(hydroxymethyl)phenol
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| Synonyms |
GW642444; GW-642444; GW 642444-X; GW642444; GW-642444; GW 642444; XGW 642444X
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.14 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 2.5 mg/mL (5.14 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.14 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
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| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.0558 mL | 10.2790 mL | 20.5579 mL | |
| 5 mM | 0.4112 mL | 2.0558 mL | 4.1116 mL | |
| 10 mM | 0.2056 mL | 1.0279 mL | 2.0558 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT06066606 | Recruiting | Drug: Placebo Drug: Vilanterol and Fluticasone Furoate (low dose) Drug: Vilanterol and Fluticasone Furoate (high dose) |
Exercise Performance | Morten Hostrup, PhD | October 5, 2023 | Not Applicable |
| NCT04522596 | Recruiting | Drug: Umeclidinium/vilanterol Other: Placebo |
Copd Heart Failure |
Luis Puente Maestu | May 21, 2021 | Phase 4 |
| NCT04536675 | Completed | Drug: Placebo Drug: Vilanterol and Umeclidinium Bromide |
Non Small Cell Lung Cancer Chronic Obstructive Pulmonary Disease |
Samsung Medical Center | April 1, 2021 | Phase 3 |
| NCT04265105 | Completed | Drug: fluticasone-vilanterol Drug: Standard Preparation |
Asthma | Royal College of Surgeons in Ireland - Medical University of Bahrain |
December 22, 2021 | Phase 2 Phase 3 |
| NCT03315000 | Completed | Drug: Fluticasone Furoate Drug: Placebos |
Asthma | University of Saskatchewan | October 13, 2017 | Phase 4 |
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