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  3. GSK656

GSK656 

目录号: HY-107775 纯度: 99.66%
产品使用指南

GSK656 是一种抗结核剂,为结核杆菌亮氨酰-tRNA 合成酶 (leucyl-tRNA synthetase (LeuRS)) 抑制剂,IC50 值为 0.2 μM。

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GSK656 Chemical Structure

GSK656 Chemical Structure

CAS No. : 2131798-13-3

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10 mg ¥8500
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50 mg ¥27000
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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

  • 实验参考方法

  • 纯度 & 产品资料

  • 参考文献

生物活性

GSK656 is a potent antitubercular agent, acting as an inhibitor of Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM.

IC50 & Target

IC50: 0.2 μM (Mtb LeuRS)[1]

体外研究
(In Vitro)

GSK656 is highly selective inhibitor for Mycobacterium tuberculosis (Mtb) leucyl-tRNA synthetase (LeuRS), with an IC50 of 0.2 μM, and shows IC50s of >300 μM and 132 μM for human mitochondrial LeuRS and human cytoplasmic LeuRS, respectively. GSK656 exhibits antitubercular activity with minimal inhibitory concentration (MIC) of 80 nM against Mtb H37Rv. GSK656 also exhibits EC50s of 381 μM against HepG2 cell, and 137 μM against HepG2 protein synthesis[1].

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

体内研究
(In Vivo)

GSK656 shows potent antitubercular activity in mice infected with M. tuberculosis H37Rv, with ED99 of 0.4 mg/kg[1].

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

分子量

293.94

Formula

C10H14BCl2NO4

CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, sealed storage, away from moisture

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

溶解性数据
In Vitro: 

DMSO : 67.5 mg/mL (229.64 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.4021 mL 17.0103 mL 34.0205 mL
5 mM 0.6804 mL 3.4021 mL 6.8041 mL
10 mM 0.3402 mL 1.7010 mL 3.4021 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 (8.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.51 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 (8.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.51 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
  • 3.

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

    Solubility: ≥ 2.5 mg/mL (8.51 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (8.51 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 25.0 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
Cell Assay
[1]

HepG2 (HB-8065) cells are cultured with fresh medium (essential minimum Eagle medium, EMEM, supplemented with 5% fetal calf serum and 2 mM l-glutamine) the day before subculturing the plates. On the day of the assay, cells (10 000 cells/well) are seeded in a black 96-well collagen coated microplate with clear bottom, except in column 11, which is dispensed only 100 mL of culture medium. Stock solution from GSK656 is prepared in 100% DMSO. Ten serial 1:2 dilutions are prepared of GSK656, and finally, a 1:200 dilution is made, in medium, to achieve a final concentration of 0.5% of DMSO. Resazurin tablets are dissolved in phosphate buffer saline at a concentration of 0.0042%. After 24 h of incubation of the cells (37°C, 5% CO2, 95% relative humidity), a volume of 150 μL of culture medium containing the appropriate test concentrations of GSK656 dilutions is added to cells in two replicates. Only 150 μL of 0.5% DMSO is added as blank control. Then, cells are exposed to GSK656 for 48 h. After that, medium is removed and resazurin solution is added to each well and incubated for further 1.5 h. Fluorescence is measured at an excitation wavelength of 515 nm and an emission wavelength of 590 nm in a Microplate reader 1420 Multilabel HTS counter, Victor 2[1].

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

Animal Administration
[1]

Mice[1]
Specific pathogen-free, 8- to 10-week-old female C57BL/6 mice are allowed to acclimate for 1 week. In brief, mice are intratracheally infected with 100 000 CFU/mouse of M. tuberculosis H37Rv. GSK656 is administered for 8 consecutive days starting 1 day after infection. For the chronic assay, mice are intratracheally infected with 100 CFU/mouse and GSK656 administered daily (7 days a week) for 8 consecutive weeks starting 6 weeks after infection. Lungs are harvested 24 h after the last administration, and all lung lobes are aseptically removed, homogenized, and frozen. Homogenates are plated onto 10% OADC-Middlebrook 7H11 medium and incubated for 21 days at 37°C. GSK656 is administered by intravenous route at 5 mg/kg single dose in saline and by oral gavage at 30 mg/kg single dose in 1% methylcellulose (1% MC). For iv route aliquots of 15 μL of blood are taken from the lateral tail vein by puncture from each mouse (n = 3) at 5, 15, and 30 min and 1, 2, 4, 8, and 24 h postdose; for oral route aliquots of 15 μL of blood are taken from the lateral tail vein by puncture from each mouse (n = 3) at 15, 30, and 45 min and 1, 2, 4, 8, and 24 h postdose[1].

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

参考文献

纯度: 99.66%

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产品名称:
GSK656
目录号:
HY-107775
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