货号	规格	价格	上海	北京	珠海	重庆	武汉
S83185-5mg	≥98%	￥830.00 S83185-5mg ￥830.00 3-5天	0 货期：3-5天	-	-	-	-
S83185-10mg	≥98%	￥1420.00 S83185-10mg ￥1420.00 3-5天	0 货期：3-5天	-	-	-	-
S83185-50mg	≥98%	￥4660.00 S83185-50mg ￥4660.00 3-5天	0 货期：3-5天	-	-	-	-

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产品描述：

GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease

靶点：

IC50: 3.2 pM (PDE4B);PDE

体外研究：

GSK256066 Trifluoroacetate is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration. GSK256066 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. GSK256066 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：

GSK256066 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.. GSK256066 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.

参考文献：

1. Tralau-Stewart CJ, et al. 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), 145-154. 2. Nials AT, et al. In vivo characterization of GSK256066, a high-affinity inhaled phosphodiesterase 4 inhibitor. J Pharmacol Exp Ther, 2011, 337(1), 137-144.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.581 ml	7.904 ml	15.808 ml
5 mM	0.316 ml	1.581 ml	3.162 ml
10 mM	0.158 ml	0.79 ml	1.581 ml
50 mM	0.032 ml	0.158 ml	0.316 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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摩尔浓度计算器

质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子摩尔量 (g/mol)

质量

浓度

体积

分子摩尔量

计算重置

GSK256066 (2,2,2-trifluoroacetic acid)