Vilanterol
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
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
- InChI
- InChI=1/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-/s3
- InChIKey
- DAFYYTQWSAWIGS-FKEMPHOKNA-N
- SMILES
- C1(O)=CC=C([C@@H](O)CNCCCCCCOCCOCC2=C(Cl)C=CC=C2Cl)C=C1CO |&1:5,r|
Vilanterol Usage And Synthesis
Uses
Vilanterol (GW642444) is a long-acting β2-adrenoceptor (β2-AR) agonist with 24 h activity. The pEC50s for β2-AR,β1-AR and β3-AR is 10.37±0.05, 6.98±0.03 and 7.36±0.03, respectively.
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].
IC 50
β adrenergic receptor
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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