公告提醒:爱必信所有产品和服务仅用于科学研究,不用于临床应用及其他用途提供产品和服务(也不为任何个人提供产品和服务)! YZ剂描述: 产品名称:GSK256066 2,2,2-trifluoroacetic acid 产品别名:6-[3-(dimethylcarbamoyl)phenyl]sulfonyl-4-(3-methoxyanilino)-8-methylquinoline-3-carboxamide,2,2,2-trifluoroacetic acid 英文别名:GSK-256066;GSK 256066 靶点:PDE CAS:1415560-64-3 纯度:>98% 外观:见爱必信官网 保存方法:store at -20℃ for one year(Powder); in DMSO or others solvent store at 2-4℃ for two weeks, at -20℃ for six months. 描述: GSK256066 is a selective PDE4B(equal affinity to isoforms A-D) inhibitor with IC50 of 3.2 pM, >380,000-fold selectivity versus PDE1/2/3/5/6 and >2500-fold selectivity against PDE4B versus PDE7. 溶解性:10 mM in DMSO 体外研究: GSK 256066 Trifluoroacetate is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration. GSK 256066 Trifluoroacetate is highly selective for PDE4, with >380,000-fold versus PDE1/2/3/5/6 and >2500-fold against PDE7, and inhibits PDE4 isoforms A-D with equal affinity. GSK 256066 Trifluoroacetate inhibits tumor necrosis factor α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC50 of 0.01 nM.
体内研究: GSK 256066 Trifluoroacetate (0.3-100 μg/kg; intratracheally) inhibits the eosinophil number increased in the bronchoalveolar lavage (BAL) in a dose-dependent fashion, in lipopolysaccharide (LPS)- and ovalbumin (OVA)-induced acute pulmonary inflammation rat models.. GSK 256066 Trifluoroacetate inhibits LPS-induced pulmonary neutrophilia, and no emetic episodes are observed in ferrets.
Animal Model: | Male Brown Norway rats(180-200 g) | Dosage: | 0.3-100 μg/kg | Administration: | Intratracheally; 30 minutes before and 6 hours after ovalbumin challenge | Result: | Inhibited the increase in eosinophil number in the BAL in a dose-dependent fashion. |
产品信息订购: 产品货号 | 产品名称 | 规格 | 价格 | 大包装及货期 | abs811662 | GSK256066 2,2,2-trifluoroacetic acid | 10mg | 2558 | 立即咨询 | 产品更多信息请进入爱必信网站咨询 |