GSK256066 Trifluoroacetate|cas:1415560-64-3|西域试剂

GSK256066 Trifluoroacetate,99.54%

产品编号：Bellancom-70069| CAS NO：1415560-64-3| 分子式：C₂₉H₂₇F₃N₄O₇S| 分子量：632.61

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货号	价格	库存与货期
Bellancom-70069	￥1300.00	杭州北京（现货）
Bellancom-70069	￥2325.00	杭州北京（现货）
Bellancom-70069	￥6696.00	杭州北京（现货）

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GSK256066 Trifluoroacetate

产品介绍

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 IC₅₀ of 3.2 pM for PDE4B. GSK256066 Trifluoroacetate is developed for the research of chronic obstructive pulmonary disease.

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.

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

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.

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

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.

体内研究

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

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 25 mg/mL (39.52 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.5808 mL	7.9038 mL	15.8075 mL
5 mM	0.3162 mL	1.5808 mL	3.1615 mL
10 mM	0.1581 mL	0.7904 mL	1.5808 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.5 mg/mL (3.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.95 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (3.95 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (3.95 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明