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GSK256066 Trifluoroacetate

目录号: PL09656 纯度: ≥99%

GSK256066 Trifluoroacetate 是一种选择性、高亲和力的 PDE 抑制剂，抑制 PDE4B 的 IC50 值为 3.2 pM。GSK256066 Trifluoroacetate 被开发用于慢性阻塞性肺病的研究。

CAS No. :1415560-64-3

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中文名称	GSK256066 Trifluoroacetate
中文别名	GSK256066 三氟乙酸盐;化合物 T11483
英文名称	GSK256066 Trifluoroacetate
英文别名	GSK256066 (2,2,2-trifluoroacetic acid);6-[3-(dimethylcarbamoyl)phenyl]sulfonyl-4-(3-methoxyanilino)-8-methylquinoline-3-carboxamide,2,2,2-trifluoroacetic acid;GSK 256066;6-[[3-[(Dimethylamino)carbonyl]phenyl]sulfonyl]-4-[(3-methoxyphenyl)amino]-8-methyl-3-quinolinecarboxamide 2,2,2-trifluoroacetate (1:1);GSK256066 Trifluoroacetate;GSK-256066 (2,2,2-trifluoroacetic acid);GSK256066 trifluoroacetate;GSK-256066; GSK 256066;2-trifluoroacetic acid);GSK256066 (2
Cas No.	1415560-64-3
分子式	C₂₉H₂₇F₃N₄O₇S
分子量	632.61
包装储存	4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
详情描述	GSK256066 Trifluoroacetate 是一种选择性、高亲和力的 PDE 抑制剂，抑制 PDE4B 的 IC50 值为 3.2 pM。GSK256066 Trifluoroacetate 被开发用于慢性阻塞性肺病的研究。

产品详情

GSK256066 Trifluoroacetate 是一种选择性、高亲和力的 PDE 抑制剂，抑制 PDE4B 的 IC₅₀ 值为 3.2 pM。GSK256066 Trifluoroacetate 被开发用于慢性阻塞性肺病的研究。

生物活性

GSK256066 Trifluoroacetate is a selective and high-affinity phosphodiesterase 4 (PDE) inhibitor, with an IC 50 of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease.

性状

Solid

IC50 & Target[1][2]

IC50: 3.2 pM (PDE4B)

体外研究(In Vitro)

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究(In Vivo)

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moistur In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

ClinicalTrial

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.

溶解度数据	In Vitro: DMSO : 25 mg/mL (39.52 mM; Need ultrasonic)配制储备液

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Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

GSK256066 Trifluoroacetate

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