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Vilanterol trifenatate is a long-acting agonist of β2-adrenoceptor (β2-AR) with inherent 24-hour activity(β2-AR, β1-AR and β3-AR pEC50s of 10.37, 6.98 and 7.36, respectively)
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $31 | In Stock | |
5 mg | $85 | In Stock | |
10 mg | $126 | In Stock | |
25 mg | $230 | In Stock | |
50 mg | $369 | In Stock | |
100 mg | $531 | In Stock | |
1 mL x 10 mM (in DMSO) | $108 | In Stock |
Description | Vilanterol trifenatate is a long-acting agonist of β2-adrenoceptor (β2-AR) with inherent 24-hour activity(β2-AR, β1-AR and β3-AR pEC50s of 10.37, 6.98 and 7.36, respectively) |
Targets&IC50 | β3-adrenoceptor:7.36±0.03(pEC50), β1-adrenoceptor:6.98±0.03(pEC50) , β2-adrenoceptor:10.37±0.05(pEC50) |
In vivo | The preclinical pharmacological profile of vilanterol using radioligand binding and cAMP studies in recombinant assays as well as human and guinea pig tissue systems to characterize β(2)-AR binding and functional properties.?Vilanterol displayed a subnanomolar affinity for the β(2)-AR that was comparable with that of salmeterol but higher than olodaterol, formoterol, and indacaterol.?In cAMP functional activity studies, vilanterol demonstrated similar selectivity as salmeterol for β(2)- over β(1)-AR and β(3)-AR, but a significantly improved selectivity profile than formoterol and indacaterol.?Vilanterol also showed a level of intrinsic efficacy that was comparable to indacaterol but significantly greater than that of salmeterol. |
Alias | GW642444 (trifenatate) |
Molecular Weight | 774.77 |
Formula | C44H49Cl2NO7 |
Cas No. | 503070-58-4 |
Smiles | OCc1cc(ccc1OC(=O)C(c1ccccc1)(c1ccccc1)c1ccccc1)[C@@H](O)CNCCCCCCOCCOCc1c(Cl)cccc1Cl |
Relative Density. | no data available |
Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature. | |||||||||||||||||||||||||||||||||||
Solubility Information | DMSO: 100 mg/mL (129.07 mM), Sonication is recommended. | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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