1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. GSK256066

GSK256066 

目录号: HY-10469 纯度: 98.83%
产品使用指南

GSK256066 是一种选择性、高亲和力的 PDE4 抑制剂,抑制 PDE4B 的 IC50 值为 3.2 pM。GSK256066 被开发用于慢性阻塞性肺病的研究。

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GSK256066 Chemical Structure

GSK256066 Chemical Structure

CAS No. : 801312-28-7

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MCE 顾客使用本产品发表的 1 篇科研文献

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK256066 is a selective and high-affinity phosphodiesterase 4 (PDE4) inhibitor, with an IC50 of 3.2 pM for PDE4B. GSK256066 is developed for the research of chronic obstructive pulmonary disease[1].

IC50 & Target[1]

PDE4

3.2 pM (IC50)

体外研究
(In Vitro)

GSK256066 is an exceptionally high-affinity inhibitor of PDE4 designed for inhaled administration[1].
GSK256066 is highly selective for PDE4, with >380,000-fold versus PDE1/2/3/5/6 and >2500-fold against PDE7[1].
GSK256066 inhibits PDE4 isoforms A-D with equal affinity (PDE4B: pIC50≥ 11.5, PDE4A: pIC50≥11.31, PDE4C: pIC50≥11.42, PDE4D: pIC50≥11.94)[1].
GSK256066 inhibits TNF-α production by lipopolysaccharide (LPS)-stimulated human peripheral blood monocytes with IC50 of 0.01 nM[1].

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

体内研究
(In Vivo)

GSK256066 (10 μg/kg; i.t.) causes significant inhibition of LPS-induced pulmonary neutrophilia[2].
GSK256066 also inhibits LPS-induced increases in exhaled nitric oxide (ED50=92 μg/kg)[2].
GSK256066 inhibits pulmonary eosinophilia in rats exposed to ovalbumin (ED50=0.4 μg/kg)[2].

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

Animal Model: Male Brown Norway rats (180-200 g)[2]
Dosage: 10 μg/kg
Administration: Intratracheal injection; before (36 hours, 24 hours, 18 hours, 12 hours, 6 hours, and 2 hours) and after (0 hour, 2 hours) LPS challenge
Result: Inhibited the LPS-induced pulmonary neutrophilia.
Clinical Trial
分子量

518.58

Formula

C27H26N4O5S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 25 mg/mL (48.21 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.9283 mL 9.6417 mL 19.2834 mL
5 mM 0.3857 mL 1.9283 mL 3.8567 mL
10 mM 0.1928 mL 0.9642 mL 1.9283 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。-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。

参考文献
  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

质量   浓度   体积   分子量 *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
C1   V1   C2   V2

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产品名称:
GSK256066
目录号:
HY-10469
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