1. GPCR/G Protein
    Neuronal Signaling
  2. Adrenergic Receptor
  3. Vilanterol trifenatate

Vilanterol trifenatate (Synonyms: GW642444 trifenatate)

Cat. No.: HY-14300A Purity: 99.20%
Handling Instructions

Vilanterol trifenatate (GW642444 trifenatate) is a long-acting β2-adrenoceptor2-AR) agonist with inherent 24-hour activity. The pEC50s for β2-AR, β1-AR and β3-AR are 10.37, 6.98 and 7.36, respectively.

For research use only. We do not sell to patients.

Vilanterol trifenatate Chemical Structure

Vilanterol trifenatate Chemical Structure

CAS No. : 503070-58-4

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10 mM * 1 mL in DMSO USD 128 In-stock
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10 mg USD 150 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Vilanterol trifenatate:

Top Publications Citing Use of Products

    Vilanterol trifenatate purchased from MCE. Usage Cited in: Mental Health and Neuroscience Institute. University of Alberta. 2016 Sep.

    The objective of the next set of experiments is to determine if the (i) super long-acting 2-AR agonists Indacaterol and Vilanterol inhibit TNF-α in a β-arrestin2-dependent manner, and (ii) whether β-arrestin2 is involved in the anti-inflammatory conversion leading to the up-regulation of IL-10 production by these β2-AR agonists.

    Vilanterol trifenatate purchased from MCE. Usage Cited in: Centre for Neuroscience. University of Alberta. 2016.

    β-arrestin2 is important in the β2-AR agonist-mediated inhibition of TNF-β, but not in β2-AR agonist-mediated IL-10 enhancement. Western blot showing silencing β-arrestin2 expression.
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    Description

    Vilanterol trifenatate (GW642444 trifenatate) is a long-acting β2-adrenoceptor2-AR) agonist with inherent 24-hour activity. The pEC50s for β2-AR, β1-AR and β3-AR are 10.37, 6.98 and 7.36, respectively.

    IC50 & Target

    pEC50: 10.37±0.05 (β2-adrenoceptor), 6.98±0.03 (β1-adrenoceptor), 7.36±0.03 (β3-adrenoceptor)[1]

    In Vitro

    The selectivity of Vilanterol trifenatate 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[1]. 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[2]. 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[3].

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

    Clinical Trial
    Molecular Weight

    774.77

    Formula

    C₄₄H₄₉Cl₂NO₇

    CAS No.
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 6 months
    -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (129.07 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.2907 mL 6.4535 mL 12.9071 mL
    5 mM 0.2581 mL 1.2907 mL 2.5814 mL
    10 mM 0.1291 mL 0.6454 mL 1.2907 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (3.23 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

      Solubility: 2.5 mg/mL (3.23 mM); Suspended solution; Need ultrasonic

    • 3.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (3.23 mM); Clear solution

    *All of the co-solvents are provided by MCE.
    References
    Kinase Assay
    [1]

    Saturation, association, and dissociation binding studies are performed for [3H]Vilanterol to determine receptor binding kinetics at the β2-AR (equilibrium dissociation constant (KD), total number of receptors (Bmax), association rate (kon), and dissociation rate (koff) are calculated). For saturation binding, membranes (in a volume of 1.4 mL to avoid ligand depletion) are incubated with increasing concentrations of [3H]Vilanterol (~0.01-1.3 nM) for 5 h before filtration. For association binding, membranes are incubated with different concentrations of [3H]Vilanterol (~0.1-1.9 nM) for varying incubation times up to 1 h before filtration. For dissociation binding, membranes are preincubated for 1 h with a fixed concentration of [3H]Vilanterol (~1.1 nM) before dissociation is initiated by a 1:20 dilution in binding buffer (containing 10 μM cold Vilanterol) and then incubated for varying times up to 8 h before filtration. Saturation binding is also completed for [3H]CGP12177 (increasing concentrations of ~0.01-2.8 nM) in the same format as described above for [3H]Vilanterol. To determine the affinity of β2-AR agonists and antagonists, competition binding displacement studies are completed 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. All competition binding displacement studies are completed in the presence of 100 µM Gpp(NH)p to ensure that binding curves are monophasic[1].

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

    References

    Purity: 99.20%

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    Product Name:
    Vilanterol trifenatate
    Cat. No.:
    HY-14300A
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