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| | 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide Basic information |
| | 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide Chemical Properties |
| 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) |
| | 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide Usage And Synthesis |
| 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. |
| | 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide Preparation Products And Raw materials |
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![6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide Structure](CAS2/GIF/801312-28-7.gif)
