1. Metabolic Enzyme/Protease
  2. Phosphodiesterase (PDE)
  3. GSK356278

GSK356278 

目录号: HY-106003 纯度: 99.89%
产品使用指南

GSK356278 是一种有效,选择性,具有口服活性和可透过血脑屏障的磷酸二酯酶 4 (PDE4) 抑制剂,对人 PDE4A,PDE4B 和 PDE4D 的 pIC50 值分别为 8.6、8.8 和 8.7。GSK356278 具有抗炎活性,并具有抗焦虑和增强认知的作用。

MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务

我们将采用定制合成服务的方式为您快速提供所需产品和技术服务

GSK356278 Chemical Structure

GSK356278 Chemical Structure

CAS No. : 720704-34-7

1.  客户无需承担相应的运输费用。

2.  同一机构(单位)同一产品试用装仅限申领一次,同一机构(单位)一年内

     可免费申领三个不同产品的试用装。

3.  试用装只面向终端客户

规格 价格 是否有货 数量
5 mg ¥1500
In-stock
10 mg ¥2500
In-stock
50 mg   询价  
100 mg   询价  

* Please select Quantity before adding items.

Customer Review

注册 MCE会员完成审核
即刻享有 积分商城 300 专属积分

Top Publications Citing Use of Products
  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK356278 is a potent, selective, orally bioavailable and brain-penetrant inhibitor of phosphodiesterase 4 (PDE4), with pIC50s of 8.6, 8.8, and 8.7 for human PDE4A, PDE4B, and PDE4D, respectively. GSK356278 has anti-inflammatory activity, and exhibits anxiolytic and cognition-enhancing effects[1].

IC50 & Target[1]

PDE4A

8.6 (pIC50)

PDE4B

8.8 (pIC50)

PDE4D

8.7 (pIC50)

体外研究
(In Vitro)

GSK356278 competes with [3H]rolipram for the high affinity rolipram binding site (HARBS) with a pKi of 8.6 in a competitive filtration-binding assay to the recombinant human PDE4B2B enzyme expressed in yeast membranes[1].
GSK356278 bounds to the HARBS in rats, mice, marmosets, and ferrets with pKis of 7.9, 7.8, 8.4, and 8.5, respectively[1].
GSK356278 inhibits LPS-induced release of TNF-α in human whole blood, with a pIC50 of 7.6[1].

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

体内研究
(In Vivo)

GSK356278 (0.003-30 mg/kg; p.o.) shows anti-inflammatory activity in rodents at exposures that does not induce pica feeding[1].
GSK356278 (0.1-0.1 mg/kg; p.o.) demonstrates efficacy in a nonhuman primate model of anxiety at exposures that do not induce emesis[1].
GSK356278 (4 doses at 0.03, 0.1, 0.3, and 1.0 mg/kg for 6 weeks; p.o.) enhances performance in a nonhuman primate object retrieval test[1]. GSK356278 exhibits oral bioavailability (rat 91%, monkey 23%) and Cmax (rat 205, monkey 41 nM) following oral administration (rat 1, monkey 0.2 mg/kg)[1].
GSK356278 exhibits terminal elimination half-lives (rat 2.2, monkey 1.5 h) due to moderate blood clearance (rat 40, monkey 16 mL/min/kg) combined with volumes of distribution (rat 6.3, monkey 2.1 L/kg) following intravenous administration (rat 1, monkey 0.2 mg/kg)[1].

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

Animal Model: Male Lewis rats (320-400 g) are treated with lipopolysaccharide (LPS)[1]
Dosage: 0.003-3 mg/kg
Administration: P.o. administration 30 minutes prior to the LPS challenge
Result: Reduced the level of neutrophilia in a dose-dependent manner, with an ED50 of 0.09 mg/kg.
Animal Model: Male CD rats[1]
Dosage: 1 mg/kg (Pharmacokinetic Analysis)
Administration: I.v. and p.o. administration
Result: Oral bioavailability (91%), Cmax (205 nM), T1/2 (2.2 h).
Clinical Trial
分子量

439.53

Formula

C21H25N7O2S

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 2.5 mg/mL (5.69 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.2752 mL 11.3758 mL 22.7516 mL
5 mM 0.4550 mL 2.2752 mL 4.5503 mL
10 mM --- --- ---
*

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 (stored under nitrogen)。-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: ≥ 1.25 mg/mL (2.84 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.84 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 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: ≥ 1.25 mg/mL (2.84 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.84 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 12.5 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
  • 3.

    请依序添加每种溶剂: 10% DMSO    90% corn oil

    Solubility: ≥ 1.25 mg/mL (2.84 mM); Clear solution

    此方案可获得 ≥ 1.25 mg/mL (2.84 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。

    以 1 mL 工作液为例,取 100 μL 12.5 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

*以上所有助溶剂都可在 MCE 网站选购。
参考文献

纯度: 99.89%

  • 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

您最近查看的产品:

Your information is safe with us. * Required Fields.

   产品名称:

 

* 需求量:

* 客户姓名:

 

* Email:

* 电话:

 

* 公司或机构名称:

   留言给我们:

Bulk Inquiry

Inquiry Information

产品名称:
GSK356278
目录号:
HY-106003
需求量: