6-Mercaptopurine(Synonyms: 6-巯基嘌呤; Mercaptopurine; 6-MP)

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6-Mercaptopurine (Synonyms: 6-巯基嘌呤; Mercaptopurine; 6-MP) 纯度: 99.16%

6-Mercaptopurine 是一种嘌呤类似物,是内源性嘌呤的拮抗剂且已被广泛用作抗白血病药物和免疫抑制药物。

6-Mercaptopurine(Synonyms: 6-巯基嘌呤; Mercaptopurine;  6-MP)

6-Mercaptopurine Chemical Structure

CAS No. : 50-44-2

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生物活性

6-Mercaptopurine is a purine analogue which acts as an antagonist of the endogenous purines and has been widely used as antileukemic agent and immunosuppressive drug.

IC50 & Target

Human Endogenous Metabolite

 

体外研究
(In Vitro)

6-Mercaptopurine hydrate (6-MP) induces NR4A3 transcriptional activity 1.6- to 11-fold (P<0.01) in a dose-responsive manner. It is found that 6-Mercaptopurine hydrate leads to a dose-dependent increase in NR4A3 protein levels. 6-MP treatment increases cell surface GLUT4 in both basal cells 1.8- to 3.6-fold (P<0.01) and insulin-stimulated cells 2.9- to 4.4-fold (P<0.01) over that in controls. It is also found that 6-Mercaptopurine hydrate increases phospho-AS160 significantly in a dose-responsive manner under both basal and insulin-stimulated conditions[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

体内研究
(In Vivo)

In the fetal telencephalons of the 6-Mercaptopurine hydrate (6-MP)-treated group, the S phase cell population increases at 36 and 48 h and returns to the control level at 72 h after treatment. The G2/M phase cell population begins to increase at 24 h, peaks at 36 h, decreases at 48 h, and finally returnes to the control level at 72 h. On the other hand, the sub-G1 phase cell population (apoptotic cells) begins to increase at 36 h, peaks at 48 h, and then decreases at 72 h[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

分子量

152.18

Formula

C5H4N4S

CAS 号

50-44-2

中文名称

6-巯基嘌呤

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

溶解性数据
In Vitro: 

DMSO : 35.71 mg/mL (234.66 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 6.5712 mL 32.8558 mL 65.7117 mL
5 mM 1.3142 mL 6.5712 mL 13.1423 mL
10 mM 0.6571 mL 3.2856 mL 6.5712 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 (protect from light)。-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: 50% PEG300    50% saline

    Solubility: 3.33 mg/mL (21.88 mM); Suspended solution; Need ultrasonic

  • 2.

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

    Solubility: ≥ 2.5 mg/mL (16.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (16.43 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

  • 3.

    请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (16.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (16.43 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
  • 4.

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

    Solubility: ≥ 2.5 mg/mL (16.43 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (16.43 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 上海金畔生物科技有限公司 网站选购。
参考文献
  • [1]. Sahasranaman S, et al. Clinical pharmacology and pharmacogenetics of thiopurines. Eur J Clin Pharmacol. 2008 Aug;64(8):753-67.

    [2]. Liu Q, et al. 6-Mercaptopurine augments glucose transport activity in skeletal muscle cells in part via a mechanism dependent upon orphan nuclear receptor NR4A3. Am J Physiol Endocrinol Metab. 2013 Nov 1;305(9):E1081-92.

    [3]. Kanemitsu H, et al. 6-Mercaptopurine (6-MP) induces cell cycle arrest and apoptosis of neural progenitor cells in the developing fetal rat brain. Neurotoxicol Teratol. 2009 Mar-Apr;31(2):104-9.

Kinase Assay
[2]

L6 myotubes are treated with DMSO control or 6-Mercaptopurine hydrate (6-MP) for 24 h, with the final 3 h of incubation including treatments in serum-free DMEM, and further incubated in the absence or presence of 100 nM insulin for 60 min at 37°C. Then, protein lysates (50 μg) are collected and subjected to SDS-PAGE and immunoblotted with primary antibodies against overnight at 4°C. The proteins are finally quantified by densitometric analysis of scanned films using Image J software[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay
[2]

Cell viability is measured using Cell Viability Assay. L6 skeletal muscle cells are seeded in 96-well plates at a density of 10,000 cells/well and differentiated into myotubes within 7 days. Cells are treated with different doses of 6-Mercaptopurine hydrate (6-MP) for 24 h before the assay. For analysis of cell viability, plates are equilibrated at room temperature for 30 min; 50 μL of Cell Titer-Glo reagent is added to each well, and plates are mixed for 12 min on an orbital shaker. Luminescence is quantified using a luminometer[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration

Around thirteen-week-old pregnant rats are used in this study. The animals are housed individually in wire-mesh cages in an air-conditioned room (temperature, 23±3°C; humidity, 50±20%; ventilation, 10 times/hour; lighting, 12 h light to12 h dark cycle) and are given pelleted diet and water ad libitum. In the experiment, fifteen pregnant rats are injected i.p. with 50 mg/kg 6-Mercaptopurine hydrate (6-MP) on E13, and three dams each are sacrificed by exsanguination from the abdominal aorta under ether anesthesia at 12, 24, 36, 48, and 72 h. Fetuses are collected from each dam by Caesarean section. As controls, fifteen pregnant rats are injected i.p. with 2.0% methylcellulose solution in distilled water at E13, and three dams are sacrificed at each of the same time-points[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

参考文献
  • [1]. Sahasranaman S, et al. Clinical pharmacology and pharmacogenetics of thiopurines. Eur J Clin Pharmacol. 2008 Aug;64(8):753-67.

    [2]. Liu Q, et al. 6-Mercaptopurine augments glucose transport activity in skeletal muscle cells in part via a mechanism dependent upon orphan nuclear receptor NR4A3. Am J Physiol Endocrinol Metab. 2013 Nov 1;305(9):E1081-92.

    [3]. Kanemitsu H, et al. 6-Mercaptopurine (6-MP) induces cell cycle arrest and apoptosis of neural progenitor cells in the developing fetal rat brain. Neurotoxicol Teratol. 2009 Mar-Apr;31(2):104-9.

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