ChemicalBook > CAS DataBase List > 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
6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide
- CAS No.801312-28-7
- Chemical Name:6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide
- CBNumber:CB42510086
- Molecular Formula:C27H26N4O5S
- Formula Weight:518.58
- MOL File:801312-28-7.mol
6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide Property
- 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
- pka 15.01±0.30(Predicted)
- form solid
- color Light yellow to yellow
- FDA UNII 2D6GK059SR
- UNSPSC Code 51111800
Safety
-
Symbol(GHS)
- Signal wordDanger
- Hazard statements H373-H335-H330
- Precautionary statements P260-P314-P501-P260-P271-P284-P304+P340-P310-P320-P403+P233-P405-P501
6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide Price
More Price(2)
- Brand: Sigma-Aldrich(India)
- Product number: SML2102
- Product name : GSK256066
- Purity:
- Packaging: 5MG
- Price: ₹8045
- Updated: 2022/06/14
- Buy: Buy
- Brand: Sigma-Aldrich(India)
- Product number: SML2102
- Product name : GSK256066
- Purity:
- Packaging: 25MG
- Price: ₹32420
- Updated: 2022/06/14
- Buy: Buy
6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide Chemical Properties,Usage,Production
- 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
- IC 50 PDE4: 3.2 pM (IC50)
-
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
Raw materials
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6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide Spectrum
801312-28-7, 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamideRelated Search:
- Inhibitors
- Inhibitor
- 抑制剂
- 代谢
- 小分子抑制剂,天然产物
- 化合物GSK256066,10 MM DMSO 溶液
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- 6-[[3-[(二甲基氨基)羰基]苯基]磺酰]-4-[(3-甲氧基苯基)氨基]-8-甲基-3-喹啉甲酰胺
- 801312-28-7
- GSK256066, 10 mM in DMSO
- 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide USP/EP/BP
- 3-Quinolinecarboxamide, 6-[[3-[(dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-
- PDE4B inhibitor GS256066
- CS-27
- 6-(3-(Dimethylcarbamoyl)phenylsulfonyl)-4-(3-methoxyphenylamino)-8-methylquinoline-3-carboxami
- GSK256066;GSK-256066;GSK 256066
- 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide GSK-256066
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- GSK2606416
- 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide
- GSK-256066