SML2102
GSK256066
동의어(들):
6-({3-[(Dimethylamino)carbonyl]phenyl}sulfonyl)-8-methyl-4-{[3-(methoxy)phenyl]amino}-3-quinolinecarboxamide, 6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide, GSK 256066, GSK-256066
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모든 사진(1)
About This Item
실험식(Hill 표기법):
C27H26N4O5S
CAS Number:
Molecular Weight:
518.58
MDL number:
UNSPSC 코드:
51111800
추천 제품
분석
≥97% (HPLC)
형태
powder
색상
white to beige
solubility
DMSO: 2 mg/mL, clear
저장 온도
−20°C
InChI
1S/C27H26N4O5S/c1-16-11-21(37(34,35)20-10-5-7-17(12-20)27(33)31(2)3)14-22-24(16)29-15-23(26(28)32)25(22)30-18-8-6-9-19(13-18)36-4/h5-15H,1-4H3,(H2,28,32)(H,29,30)
InChI key
JFHROPTYMMSOLG-UHFFFAOYSA-N
생화학적/생리학적 작용
GSK256066 is a reversible and cAMP-competitive phosphodiesterase 4 (PDE4) inhibitor that targets all PDE4 subtypes with high affinity (IC50 = 53.7 pM against 2 nM [3H]-rolipram for binding HRBS in rat brain cytosol), potency and selectivity (pIC50 ≥11.31/11.5/11.42/11.94 against PDE4A/B/C/D vs. pIC50 = 5.73/5.92/5.93/5.39/5.28/8.11 against PDE1/2/3/5/6/7 by SPA assays). GSK256066 effectively inhibits LPS-induced TNFα production from human whole blood and isolated PBMCs (pIC50 = 126 and 10 pM, respectively) in vitro and acute pulmonary neutrophilia in rats in vivo (ED50 = 1.1 μg/kg, administered intratracheally 2 hrs priror to LPS). GSK256066 is shown to be more potent than Cilomilast (SB-207499) and Roflumilast in both cell-free and cell-based assays.
Storage Class Code
11 - Combustible Solids
WGK
WGK 3
시험 성적서(COA)
제품의 로트/배치 번호를 입력하여 시험 성적서(COA)을 검색하십시오. 로트 및 배치 번호는 제품 라벨에 있는 ‘로트’ 또는 ‘배치’라는 용어 뒤에서 찾을 수 있습니다.
Anthony T Nials et al.
The Journal of pharmacology and experimental therapeutics, 337(1), 137-144 (2011-01-06)
Oral phosphodiesterase (PDE) 4 inhibitors have demonstrated clinical efficacy in chronic obstructive pulmonary disease and asthma. Preclinical and clinical investigation of inhaled PDE4 inhibitors is ongoing. 6-({3-[(Dimethylamino)carbonyl]phenyl}sulfonyl)-8-methyl-4-{[3-methyloxy)phenyl]amino}-3-quinolinecarboxamide (GSK256066) is an exceptionally high-affinity and selective inhibitor of PDE4 designed for inhaled
Seamus Grundy et al.
Respiratory research, 17, 9-9 (2016-01-27)
CD8 lymphocytes play an important role in the pathogenesis of COPD. Corticosteroids and phosphodiesterase 4 (PDE4) inhibitors are anti-inflammatory drugs used for COPD treatment. Little is known of the combined effect of these drugs on COPD CD8 cells. We studied
Dave Singh et al.
Respiratory research, 11, 26-26 (2010-03-03)
GSK256066 is a selective phosphodiesterase 4 inhibitor that can be given by inhalation, minimising the potential for side effects. We evaluated the effects of GSK256066 on airway responses to allergen challenge in mild asthmatics. In a randomised, double blind, cross-over
Michael D Woodrow et al.
Bioorganic & medicinal chemistry letters, 19(17), 5261-5265 (2009-08-07)
Crystallography driven optimisation of a lead derived from similarity searching of the GSK compound collection resulted in the discovery of quinoline-3-carboxamides as highly potent and selective inhibitors of phosphodiesterase 4B. This series has been optimized to GSK256066, a potent PDE4B
Cathy J Tralau-Stewart et al.
The Journal of pharmacology and experimental therapeutics, 337(1), 145-154 (2011-01-06)
Oral phosphodiesterase (PDE) 4 inhibitors such as roflumilast have established the potential of PDE4 inhibition for the treatment of respiratory diseases. However, PDE4 inhibitor efficacy is limited by mechanism-related side effects such as emesis and nausea. Delivering the inhibitor by
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