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

Vilanterol trifenatate  (Synonyms: GW642444 trifenatate)

Cat. No.: HY-14300A Purity: 99.29%
COA Handling Instructions

Vilanterol trifenatate (GW642444 trifenatate) is a long-acting β2-adrenoceptor (β2-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 141 In-stock
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Customer Review

Based on 7 publication(s) in Google Scholar

Other Forms of Vilanterol trifenatate:

Vilanterol trifenatate Related Antibodies

Top Publications Citing Use of Products

    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.

    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.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Vilanterol trifenatate (GW642444 trifenatate) is a long-acting β2-adrenoceptor (β2-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

    β adrenergic receptor

     

    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.

    Vilanterol trifenatate Related Antibodies
    Clinical Trial
    Molecular Weight

    774.77

    Appearance

    Solid

    Formula

    C44H49Cl2NO7
    CAS No.
    SMILES

    OC1=CC=C([C@@H](O)CNCCCCCCOCCOCC2=C(Cl)C=CC=C2Cl)C=C1CO.O=C(O)C(C3=CC=CC=C3)(C4=CC=CC=C4)C5=CC=CC=C5
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (64.54 mM; ultrasonic and warming and heat to 60°C)

    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 mg/mL (2.58 mM); Clear solution; Need ultrasonic

    • 2.

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

      Solubility: 2 mg/mL (2.58 mM); Suspended solution; Need ultrasonic

    • 3.

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

      Solubility: 2 mg/mL (2.58 mM); Clear solution; Need ultrasonic

    *All of the co-solvents are available by MCE.
    Purity & Documentation

    Purity: 99.29%

    COA (249 KB) HNMR (283 KB) LCMS (93 KB)

    Handling Instructions (2659 KB)
    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
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    Vilanterol trifenatate Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    Keywords:

    Vilanterol503070-58-4GW642444GW 642444GW-642444Adrenergic ReceptorBeta ReceptorInhibitorinhibitorinhibit

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