2. GPCR/G Protein Immunology/Inflammation
  3. CCR
  4. GSK2239633A

GSK2239633A 是一种 CC 趋化因子受体4 (CCR4) 拮抗剂，抑制 [125I]-TARC 与人 CCR4 结合，pIC50 为 7.96±0.11。

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GSK2239633A Chemical Structure

GSK2239633A Chemical Structure

CAS No. : 1240516-71-5

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥1933
In-stock
1 mg ￥727
In-stock
5 mg ￥1600
In-stock
10 mg ￥2600
In-stock
25 mg ￥5500
In-stock
50 mg ￥8800
In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

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GSK2239633A 相关抗体

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

  • 生物活性

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK2239633A is a CC-chemokine receptor 4 (CCR4) antagonist, which inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96 ± 0.11.

IC50 & Target

[125I]-TARC-CCR4

7.96 (pIC50)

体外研究
(In Vitro)

The GSK2239633A is an allosteric antagonist of human CCR4. GSK2239633A inhibits the binding of [125I]-TARC to human CCR4 with a pIC50 of 7.96±0.11 and also inhibits thymus- and activation-regulated chemokine-induced (TARC)-induced increases in the F-actin content of isolated human CD4+ CCR4+ T-cells with a pA2 of 7.11±0.29[1]. The effect of GSK2239633A (Compound 3) on CCL17-induced increases in the F-actin content of human CD4+ CCR4+ T cells is measured. The pEC50 value is 8.79±0.22[2].

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

GSK2239633A 相关抗体:
体内研究
(In Vivo)

Following intravenous dosing, plasma GSK2239633A displays rapid, bi-phasic distribution and slow terminal elimination (t1/2: 13.5 hours), suggesting that GSK2239633A is a low to moderate clearance drug. Following oral dosing, blood levels of GSK2239633A reach Cmax rapidly (median tmax: 1.0-1.5 hours). Estimated GSK2239633A bioavailability is low with a maximum value determined of only 16%[1]. GSK2239633A (Compound 9) demonstrates good pharmacokinetic data in preclinical animal studies (bioavailability in rats and beagle dogs 85% and 97% respectively)[3].

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

549.06

Formula

C24H25ClN4O5S2
CAS 号
性状

固体

颜色

White to off-white

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 2 years
-20°C 1 year
溶解性数据
In Vitro: 

DMSO 中的溶解度 : ≥ 250 mg/mL (455.32 mM; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

* "≥" means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.8213 mL 9.1065 mL 18.2129 mL
5 mM 0.3643 mL 1.8213 mL 3.6426 mL
查看完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

  • 摩尔计算器

  • 稀释计算器

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

质量
=
浓度
×
体积
×
分子量 *

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

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start)

C1

×
体积 (start)

V1

=
浓度 (final)

C2

×
体积 (final)

V2

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

  • 方案 一

    请依序添加每种溶剂： 10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.08 mg/mL (3.79 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；再向上述体系中加入 50 μL Tween-80，混合均匀；然后再继续加入 450 μL 生理盐水 定容至 1 mL。

    生理盐水的配制：将 0.9 g 氯化钠，溶解于 ddH₂O 并定容至 100 mL，可以得到澄清透明的生理盐水溶液。
  • 方案 二

    请依序添加每种溶剂： 10% DMSO    90% Corn Oil

    Solubility: ≥ 2.08 mg/mL (3.79 mM); 澄清溶液

    此方案可获得 ≥ 2.08 mg/mL（饱和度未知）的澄清溶液，此方案实验周期在半个月以上的动物实验酌情使用。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

动物溶解方案计算器
请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

g

每只动物的给药体积

μL

动物数量

只
由于实验过程有损耗，建议您多配一只动物的量
请输入您的动物体内配方组成：
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
方案所需 助溶剂 包括：DMSO， ，均可在 MCE 网站选购。 ，Tween 80，均可在 MCE 网站选购。
计算结果
工作液所需浓度 : mg/mL
储备液配制方法 : mg 药物溶于 μL  DMSO（母液浓度为 mg/mL）。
您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。
动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。
连续给药周期超过半月以上，请谨慎选择该方案。
请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热 （超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。
纯度 & 产品资料

纯度: 99.86%

COA (205 KB) LCMS (267 KB)

产品使用指南 (1538 KB)
参考文献
Cell Assay
[2]

Blood is taken from normal volunteers who have taken no medication within the previous 10 days and chemokine-induced increases in the filamentous (F)-actin content of CD4+ CCR4+ T cells are measured. Briefly, the peripheral blood mononuclear cells (PBMC) are isolated and stained with fluorescein isothiocyanate-conjugated anti-human CD4 and phycoerythrin-conjugated anti-CCR4 antibodies. The cells are then incubated with GSK2239633A (1 μM) or vehicle (0.1% DMSO) for 30 min at 37°C before stimulation with agonist for 15 sec. The assay is terminated by addition of 3% formaldehyde. The fixed cells are stained with Alexa fluor-647 phalloidin and the mean fluorescence intensity of 1000 CD4+ CCR4+ cells per sample is determined. This is expressed as a fraction of the mean intensity of the CD4+ CCR4- cells in the same sample[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration
[3]

Rats and Dogs[3]
Pharmacokinetics are determined in male Wistar Han rats (277-305 g) or male Sprague Dawley (crl:CD(SD)) rats 277-305 g) and male Beagle dogs (14-16 kg; aged approximately 3-4 years) following single oral and intravenous administration to aid prediction of the likely human pharmacokinetics using precedented physiological scaling techniques. In the rat, compounds (e.g., GSK2239633A) are dosed intravenously and orally to 2 rats per compound per route. Nominal doses of 1 mg/kg are used for intravenous (iv) and oral (po) administration and studies are conducted following routine animal husbandry methods. Rats are housed in standard holding cages and maintained in a controlled environment with free access to food and water. Serial blood samples are collected via a temporary cannula inserted into the tail vein of all animals. For the intravenously dosed animals the cannula is inserted into a vein discrete from that used for dosing. The dogs are kept in slings for no longer than 2 h following the end of dosing on each phase of the study. Compounds (e.g., GSK2239633A) are dosed intravenously (bolus, 0.5 mg/kg) using an angiocath and orally (gavage; 1 mg/kg) to two male Beagle dogs per compound in a cross over design. Serial blood samples are collected from the cephalic vein via an angiocath for the first 2 h post dose and via direct venipuncture for the remainder of the study.

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

GSK2239633A 相关分类

完整储备液配制表

* 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, 2 years; -20°C, 1 year。-80°C储存时，请在2年内使用， -20°C储存时，请在1年内使用。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 1.8213 mL 9.1065 mL 18.2129 mL 45.5324 mL
5 mM 0.3643 mL 1.8213 mL 3.6426 mL 9.1065 mL
10 mM 0.1821 mL 0.9106 mL 1.8213 mL 4.5532 mL
15 mM 0.1214 mL 0.6071 mL 1.2142 mL 3.0355 mL
20 mM 0.0911 mL 0.4553 mL 0.9106 mL 2.2766 mL
25 mM 0.0729 mL 0.3643 mL 0.7285 mL 1.8213 mL
30 mM 0.0607 mL 0.3035 mL 0.6071 mL 1.5177 mL
40 mM 0.0455 mL 0.2277 mL 0.4553 mL 1.1383 mL
50 mM 0.0364 mL 0.1821 mL 0.3643 mL 0.9106 mL
60 mM 0.0304 mL 0.1518 mL 0.3035 mL 0.7589 mL
80 mM 0.0228 mL 0.1138 mL 0.2277 mL 0.5692 mL
100 mM 0.0182 mL 0.0911 mL 0.1821 mL 0.4553 mL
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

GSK2239633A1240516-71-5CCRCC chemokine receptorInhibitorinhibitorinhibit

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