| Identification | More | [Name]
GSK256066 | [CAS]
801312-28-7 | [Synonyms]
GSK-256066
GSK2606416
6-(3-(dimethylcarbamoyl)phenylsulfonyl)-4-(3-methoxyphenylamino)-8-methylquinoline-3-carboxamide
6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide
6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide GSK-256066 | [Molecular Formula]
C27H26N4O5S | [MDL Number]
MFCD18206923 | [MOL File]
801312-28-7.mol | [Molecular Weight]
518.584 |
| Chemical Properties | Back Directory | [Boiling point ]
791.7±60.0 °C(Predicted) | [density ]
1.345 | [storage temp. ]
Store at -20°C,unstable in solution, ready to use. | [solubility ]
insoluble in DMSO; insoluble in EtOH; insoluble in H2O | [form ]
solid | [pka]
15.01±0.30(Predicted) | [color ]
Light yellow to yellow |
| Hazard Information | Back Directory | [Usage]
Quinoline derivative and a potential selective PDE4 phosphodiesterase inhibitor to treat prophylaxis or treatment of clinical conditions such as inflammatory or allergic diseases. | [Uses]
Quinoline derivative and a potential selective PDE4 phosphodiesterase inhibitor to treat prophylaxis or treatment of clinical conditions such as inflammatory or allergic diseases. | [Biological Activity]
apparent ic50 3.2 pm, steady state ic50 < 0.5 pmgsk256066 is an exceptionally high-affinity and selective inhibitor of pde4 designed for inhaled delivery.oral phosphodiesterase (pde) 4 inhibitors have demonstrated clinical efficacy in chronic obstructive pulmonary disease and asthma. | [in vitro]
gsk256066 is a slow- and tight-binding inhibitor of pde4b, more potent than any previously documented compound, for example roflumilast, tofimilast and cilomilast [1]. | [in vivo]
when administered by the intratracheal route to rats, gsk256066 inhibited lps-induced pulmonary neutrophilia with ed50s of 1.1 μg/kg (aqueous suspension) and 2.9 μg/kg (dry powder formulation) and was more potent than an aqueous suspension of the corticosteroid fluticasone propionate (ed50 9.3 μg/kg) [1]. | [target]
PDE4 | [References]
[1] tralau-stewart cj, williamson ra, nials at, gascoigne m, dawson j, hart gj, angell ad, solanke ye, lucas fs, wiseman j, ward p, ranshaw le, knowles rg. gsk256066, an exceptionally high-affinity and selective inhibitor of phosphodiesterase 4 suitable for administration by inhalation: in vitro, kinetic, and in vivo characterization. j pharmacol exp ther. 2011;337(1):145-54.
[2] watz h, mistry sj, lazaar al; ipc101939 investigators. safety and tolerability of the inhaled phosphodiesterase 4 inhibitor gsk256066 in moderate copd. pulm pharmacol ther. 2013;26(5):588-95. |
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