1. Apoptosis
  2. Apoptosis
  3. Azathioprine

Azathioprine  (Synonyms: 硫唑嘌呤; BW 57-322)

目录号: HY-B0256 纯度: 99.98%
COA 产品使用指南

Azathioprine (BW 57-322) 是一种具有口服活性的免疫抑制剂 (immunosuppressive agent)。硫唑嘌呤在体内可以转化为活性代谢物 6-巯基嘌呤( 6-MP ),具有骨髓抑制作用,可诱导细胞凋亡 (apoptosis)。

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Azathioprine Chemical Structure

Azathioprine Chemical Structure

CAS No. : 446-86-6

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥500
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500 mg ¥400
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1 g ¥530
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5 g ¥950
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Other Forms of Azathioprine:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Azathioprine (BW 57-322) is an orally active immunosuppressive agent. Azathioprine can be converted in vivo to the active metabolite 6-mercaptopurine (6-MP). Azathioprine has myelosuppressive effects and induces apoptosis[1][3].

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
B-cell IC50
2.7 μg/mL
Compound: azathioprine
Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay
[PMID: 14738397]
Lymphocyte IC50
2.9 μg/mL
Compound: Azathioprine
Immunosuppressive activity in baboon lymphocytes by mixed lymphocyte reaction assay
Immunosuppressive activity in baboon lymphocytes by mixed lymphocyte reaction assay
[PMID: 3373220]
Lymphocyte IC50
3 μg/mL
Compound: Azathioprine
Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay
Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay
[PMID: 3373220]
PBMC IC50
230.4 nM
Compound: azathioprine
Inhibition of T cell mitogen-induced blastogenesis in human PBMC after 4 days
Inhibition of T cell mitogen-induced blastogenesis in human PBMC after 4 days
[PMID: 18467007]
T-cell IC50
2.7 μg/mL
Compound: azathioprine
Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay
[PMID: 14738397]
体外研究
(In Vitro)

Azathioprine (0-50 μM, 48 hours) can induce severe intracellular GSH depletion with relevant concentrations in both primary rat and human hepatocytes[2].

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

Cell Viability Assay[2]

Cell Line: Rat hepatocytes, Human hepatocytes
Concentration: 0-50 μM
Incubation Time: 24-48 hours
Result: Showed the decrease in cell viability and intracellular GSH levels in rat hepatocytes as low concentration of 0.5 μM but no significant decrease in cell viability at concentrations below 50 μM as well as GSH depletion was obviously noted at a concentration as low as 1 μM in human hepatocytes.
体内研究
(In Vivo)

Azathioprine (oral gavage, 25-400 mg/kg, everyday, 10days) can affect bone marrow cells, red blood cells, and peripheral blood cytokines and other related parameters in a dose-dependent manner, and can induce apoptosis in female CD-1 mice and ICR mice[3].

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

Animal Model: Outbred female CD-1 mice, Female ICR mice[3]
Dosage: 25-400 mg/kg
Administration: Oral gavage; everyday; 10days
Result: Induced a decrease in erythrocyte-related parameters as well as leukocyte-related parameters in a dose-dependent manner.
Induced 52.4%, 35.4%, 17.9%, 16.1% and 15.2% reduction in bone marrow cells at concentrations of 40, 60, 80, 100 and 120 mg/kg, respectively while fms-like tyrosine kinase-3(FLT-3) ligand (FL)-related cytokines were increased.
Clinical Trial
分子量

277.26

Formula

C9H7N7O2S

CAS 号
性状

固体

颜色

Light yellow to yellow

中文名称

依木兰;咪唑硫嘌呤;硫唑嘌呤

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
细胞实验: 

DMSO 中的溶解度 : 50 mg/mL (180.34 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 3.6067 mL 18.0336 mL 36.0672 mL
5 mM 0.7213 mL 3.6067 mL 7.2134 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, 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。

  • 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

动物实验:

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 (7.50 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。

    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% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.08 mg/mL (7.50 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。

    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 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

    2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。
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

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)。

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

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: 99.98%

参考文献

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, 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。

可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.6067 mL 18.0336 mL 36.0672 mL 90.1681 mL
5 mM 0.7213 mL 3.6067 mL 7.2134 mL 18.0336 mL
10 mM 0.3607 mL 1.8034 mL 3.6067 mL 9.0168 mL
15 mM 0.2404 mL 1.2022 mL 2.4045 mL 6.0112 mL
20 mM 0.1803 mL 0.9017 mL 1.8034 mL 4.5084 mL
25 mM 0.1443 mL 0.7213 mL 1.4427 mL 3.6067 mL
30 mM 0.1202 mL 0.6011 mL 1.2022 mL 3.0056 mL
40 mM 0.0902 mL 0.4508 mL 0.9017 mL 2.2542 mL
50 mM 0.0721 mL 0.3607 mL 0.7213 mL 1.8034 mL
60 mM 0.0601 mL 0.3006 mL 0.6011 mL 1.5028 mL
80 mM 0.0451 mL 0.2254 mL 0.4508 mL 1.1271 mL
100 mM 0.0361 mL 0.1803 mL 0.3607 mL 0.9017 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.

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Azathioprine
目录号:
HY-B0256
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