ChemicalBook Produktkatalog Bio- und Chemieingenieurwesen Inhibitoren Stoffwechsel PDE-Inhibitoren 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 Struktur

6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide

Bezeichnung:6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide

CAS-Nr801312-28-7

Englisch Name:6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide

CBNumberCB42510086

SummenformelC27H26N4O5S

Molgewicht518.58

MOL-Datei801312-28-7.mol

6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide physikalisch-chemischer Eigenschaften

Siedepunkt	791.7±60.0 °C(Predicted)
Dichte	1.345
storage temp.	Store at -20°C,unstable in solution, ready to use.
Löslichkeit	insoluble in DMSO; insoluble in EtOH; insoluble in H2O
pka	15.01±0.30(Predicted)
Aggregatzustand	solid
Farbe	Light yellow to yellow

Gefahreninformationscode (GHS)

6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide Chemische Eigenschaften,Einsatz,Produktion Methoden

Verwenden
Quinoline derivative and a potential selective PDE4 phosphodiesterase inhibitor to treat prophylaxis or treatment of clinical conditions such as inflammatory or allergic diseases.
Biologische Aktivität
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
Einzelnachweise
[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 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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