1. Metabolic Enzyme/Protease Immunology/Inflammation
  2. Ser/Thr Protease Thrombopoietin Receptor
  3. Imidazole

Imidazole  (Synonyms: 咪唑; Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene)

目录号: HY-D0837 纯度: 99.94%
COA 产品使用指南 技术支持

Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene),一种杂环芳香族化合物。咪唑类分子已被用作缓蚀剂、乙酰胆碱酯酶(AChEI)和黄嘌呤氧化酶(XO)抑制剂,具有抗真菌、抗结核、抗炎、抗氧化、镇痛等生物活性。咪唑抑制血小板微粒体将内过氧化物(PGG2 和PGH2)转化为血栓素A2。咪唑衍生物对 SARS-CoV-2 3ClPro 酶有抑制作用,有望用于阿尔茨海默病、痛风、新冠肺炎和血栓疾病领域的研究。

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Imidazole Chemical Structure

Imidazole Chemical Structure

CAS No. : 288-32-4

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规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥193
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5 g ¥175
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10 g ¥266
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25 g ¥462
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50 g ¥602
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100 g ¥784
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Other Forms of Imidazole:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

Imidazole (Glyoxaline; 1,3-Diaza-2,4-cyclopentadiene) is a heterocyclic aromatic compound. Imidazole bearing molecules have been used as corrosion, acetylcholinesterase (AChEI) and xanthine oxidase (XO) inhibitors, performing biological activities such as antifungal, antituberculosis, anti-inflammatory, antioxidant, and analgesic, amongst many others. Imidazole inhibits the enzymatic conversion of the endoperoxides (PGG2 and PGH2) to thromboxane A2 by platelet microsomes. Imidazole derivatives exhibits inhibition on SARS-CoV-2 3CLPro enzyme, which is promising for research in the field of Alzheimer’s disease, gout, COVID-19 and thrombo-embolic disease[1][2][3].

IC50 & Target

Human Endogenous Metabolite

 

细胞效力
(Cellular Effect)
Cell Line Type Value Description References
A549 IC50
> 20 μM
Compound: Imidazole
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
[PMID: 30822712]
A549 IC50
> 20 μM
Compound: Imidazole
Cytotoxicity against human A549 cells by MTT assay
Cytotoxicity against human A549 cells by MTT assay
[PMID: 26684853]
CHO IC50
3675 μM
Compound: 20
Cytotoxicity against CHO cells after 48 hrs by MTT assay
Cytotoxicity against CHO cells after 48 hrs by MTT assay
[PMID: 20634079]
HL-60 IC50
> 20 μM
Compound: Imidazole
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Antiproliferative activity against human HL60 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
[PMID: 30822712]
HL-60 IC50
> 20 μM
Compound: Imidazole
Cytotoxicity against human HL60 cells by MTT assay
Cytotoxicity against human HL60 cells by MTT assay
[PMID: 26684853]
MCF7 IC50
> 20 μM
Compound: Imidazole
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
[PMID: 30822712]
MCF7 IC50
> 20 μM
Compound: Imidazole
Cytotoxicity against human MCF7 cells by MTT assay
Cytotoxicity against human MCF7 cells by MTT assay
[PMID: 26684853]
SMMC-7721 IC50
> 20 μM
Compound: Imidazole
Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Antiproliferative activity against human SMMC7721 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
[PMID: 30822712]
SMMC-7721 IC50
> 20 μM
Compound: Imidazole
Cytotoxicity against human SMMC7721 cells by MTT assay
Cytotoxicity against human SMMC7721 cells by MTT assay
[PMID: 26684853]
SW480 IC50
> 20 μM
Compound: Imidazole
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
Antiproliferative activity against human SW480 cells assessed as reduction in cell viability incubated for 48 hrs by MTS assay
[PMID: 30822712]
SW480 IC50
> 20 μM
Compound: Imidazole
Cytotoxicity against human SW480 cells by MTT assay
Cytotoxicity against human SW480 cells by MTT assay
[PMID: 26684853]
体外研究
(In Vitro)

Imidazole (0.01-100 μM, 48 h) 无抑制活性,但咪唑衍生物对不同肿瘤细胞系均有显著抑制作用[1]
Imidazole (0.01-100 μM, 48 h) 对肿瘤细胞中 EGFR 和 HER2 均有较弱的亲和力,而咪唑衍生物可提高其对肿瘤细胞中这些受体的亲和力[1]

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

Cell Proliferation Assay[1]

Cell Line: A549, HBL-100, HeLa, SW1573, T-47D, WiDr cell lines
Concentration: 0.01-100 μM
Incubation Time: 48 h
Result: Had no inhibitory activity in the compounds employed as control in different tumor cell lines.
体内研究
(In Vivo)

Imidazole (50 pg/ml , 灌注) 和类似的化合物是内过氧化物转化为血栓素的选择性抑制剂[3]

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

分子量

68.08

Formula

C3H4N2

CAS 号
性状

固体

颜色

Off-white to light brown

中文名称

咪唑;异吡唑;间二氮茂

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Store at room temperature 3 years

In solvent -80°C 2 years
-20°C 1 year
溶解性数据
细胞实验: 

DMSO 中的溶解度 : 100 mg/mL (1468.86 mM; 超声助溶 (<60°C); 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 14.6886 mL 73.4430 mL 146.8860 mL
5 mM 2.9377 mL 14.6886 mL 29.3772 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

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: ≥ 2.5 mg/mL (36.72 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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;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: ≥ 2.5 mg/mL (36.72 mM); 澄清溶液

    此方案可获得 ≥ 2.5 mg/mL(饱和度未知)的澄清溶液。

    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。

    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。

以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: PBS

    Solubility: 100 mg/mL (1468.86 mM); 澄清溶液; 超声助溶

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)。
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: 99.94%

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, 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 14.6886 mL 73.4430 mL 146.8860 mL 367.2150 mL
5 mM 2.9377 mL 14.6886 mL 29.3772 mL 73.4430 mL
10 mM 1.4689 mL 7.3443 mL 14.6886 mL 36.7215 mL
15 mM 0.9792 mL 4.8962 mL 9.7924 mL 24.4810 mL
20 mM 0.7344 mL 3.6722 mL 7.3443 mL 18.3608 mL
25 mM 0.5875 mL 2.9377 mL 5.8754 mL 14.6886 mL
30 mM 0.4896 mL 2.4481 mL 4.8962 mL 12.2405 mL
40 mM 0.3672 mL 1.8361 mL 3.6722 mL 9.1804 mL
50 mM 0.2938 mL 1.4689 mL 2.9377 mL 7.3443 mL
60 mM 0.2448 mL 1.2241 mL 2.4481 mL 6.1203 mL
80 mM 0.1836 mL 0.9180 mL 1.8361 mL 4.5902 mL
100 mM 0.1469 mL 0.7344 mL 1.4689 mL 3.6722 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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