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Vilanterol

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Vilanterol Basic information

Product Name:
Vilanterol
Synonyms:
  • Vilanterol
  • GW 642444X
  • Vilanterol API
  • GW 642444
  • GW642444
  • GW-642444
  • 4-[(R)-2-[[6-[2-(2,6-Dichlorobenzyloxy)ethoxy]hexyl]amino]-1-hydroxyethyl]-2-hydroxymethylphenol
  • Vilanterol(GW642444)
CAS:
503068-34-6
MF:
C24H33Cl2NO5
MW:
486.43
EINECS:
690-631-3
Product Categories:
  • Inhibitors
  • Intermediate
  • 503068-34-6
Mol File:
503068-34-6.mol
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Vilanterol Chemical Properties

Boiling point:
646.7±55.0 °C(Predicted)
Density 
1?+-.0.06 g/cm3(Predicted)
storage temp. 
Store at -20°C
solubility 
Soluble in DMSO
form 
solution in ethanol
pka
9.99±0.20(Predicted)
color 
Light yellow to yellow
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Vilanterol Usage And Synthesis

Definition

ChEBI: An dichlorobenzene derivative that is used in the form of its trifenate salt for treatment of chronic obstructive pulmonary disease.

Biological Activity

vilanterol is a novel and selective agonist of β2-ar with a pec50 value of 10.37±0.05 [1].vilanterol is a novel long-acting β2-ar agonist (laba) with 24h activity in development for inhaled once daily treatment. in the radioligand binding studies, vilanterol has shown the binding affinity in the one-affinity site model with pkd values of 9.44±0.07 and 10.82±0.12 in the presence gpp(nh)p and absence gpp(nh)p, respectively. in dissociation studies, vilanterol has been reported to bind from the β2-ar with a dissociation t1/2 value of 3.5 min in the presence of gpp(nh)p. vilanterol has been found to have a good selectivity for β2-ar over the other β-ar receptor subtypes(β1and β3) with pec50 values of 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively. vilanterol has exhibited at least 1000-fold selectivity over both β1-and β3-ar subtypes [1].

References

[1] slack rj1, barrett vj, morrison vs, sturton rg, emmons aj, ford aj, knowles rg.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.

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