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- 文献和实验
- 技术资料
- CAS号：
37836-90-1
- 规格：
1mg/1mLx10mM(inDMSO)/5mg/10mg/25mg/50mg/100mg/200mg
| 规格： | 1mg | 产品价格： | ￥194.0 |
|---|---|---|---|
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥633.0 |
| 规格： | 5mg | 产品价格： | ￥358.0 |
| 规格： | 10mg | 产品价格： | ￥590.0 |
| 规格： | 25mg | 产品价格： | ￥984.0 |
| 规格： | 50mg | 产品价格： | ￥1496.0 |
| 规格： | 100mg | 产品价格： | ￥2144.0 |
| 规格： | 200mg | 产品价格： | ￥3032.0 |
Product Introduction
Bioactivity
| 名称 | MPO-IN-28 |
| 描述 | MPO-IN-28 is a novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM. |
| 细胞实验 | To evaluate whether selected compounds exhibited toxicity at the cellular level at concentrations ranging from 0.005 to 50 μM, the colorimetric assay MTT was performed58 in normal human dermal fibroblasts (NHDF). Briefly, cell line was cultured in cell culture flasks, grown, and maintained at 37 °C, 95% humidity, 5% CO2 in fibroblast medium FBM supplemented with 2% fetal bovine serum, 0.1% insulin, rhFGF-B, and gentamicin and amphotericin. NHDF cells were chemically detached with trypsin and seeded in 96-well plates and left to attach for 24 h. Prior to treatment, compounds were dissolved in DMSO at a concentration of 10 mM, and cells were treated with the different concentrations of the compounds diluted in culture medium (5 nM to 50 μM) or left untreated for 72 h. The amount of viable cells was determined through the MTT mitochondrial reduction into formazan by living cells according to previously described.58 The optical density (OD) was measured in a Biorad 680RX plate reader at 570 nm (reference 630 nm), and the OD of the untreated control was normalized as 100% of viable cells, allowing determination of the concentration that inhibited their growth by 50% (IC50). |
| 激酶实验 | The assay is based on the production of taurine chloramine produced by the MPO/H2O2/Cl? system in the presence of a selected inhibitor at defined concentration. The reaction mixture contained the following reagents in a final volume of 200 μL: 10 mM phosphate buffer (pH 7.4, 300 mM NaCl), 15 mM taurine, compound to be tested (up to 20 μM), and a fixed amount of recombinant MPO (6.6 μL of MPO batch solution diluted 2.5 times, 40 nM). When necessary, the volume was adjusted with water. This mixture was incubated at 37 °C, and the reaction was initiated with 10.0 μL of H2O2 (100 μM). After 5 min, the reaction was stopped by the addition of 10 μL of catalase (8 units/μL). To determine the amount of taurine chloramine produced, 50 μL of 1.35 mM solution of thionitrobenzoic acid was added and the volume was adjusted to 300 μL with water. Then the absorbance of the solutions was measured at 412 nm with a microplate reader, and the curve of absorbance as a function of inhibitor concentration was plotted. IC50 values were then determined by standard procedures by taking into account the absence of hydrogen peroxide as 100% inhibition and the absence of inhibitors as 0% inhibition. |
| 体外活性 | 5 μM of MPO-IN-28 was added to MPO in the presence of 30 μM of guaiacol. In the absence of H2O2, there was no inhibition of MPO, clearly underlining that MPO-IN-28 is an irreversible mechanism-based inhibitor. MPO-IN-28 inhibits the growth of normal human dermal fibroblast (NHDF) at a concentration (IC50) of 17 μM, which is about 400 times higher than the concentration of the MPO inhibitory effect (0.044 μM). |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (8.65 mM), Sonication is recommended. DMSO : 22.73 mg/mL (98.29 mM), Sonication is recommended. |
| 关键字 | Myeloperoxidase | MPO-IN-28 | MPOIN28 | MPO IN 28 | MPO | Inhibitor | inhibit | GlutathionePeroxidase | Glutathione Peroxidase |
| 相关产品 | 4-Aminosalicylic acid | ML-210 | (±)-Methyl Jasmonate | 5-Aminosalicylic Acid | Probucol | Cefdinir | Melatonin | 2-Acetamidophenol | Sodium 2-mercaptoethanesulfonate | AZD8309 | 4-Methylesculetin | PF-1355 |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Bioactive Compounds Library Max | Oxidation-Reduction Compound Library | Metabolism Compound Library | Anti-Aging Compound Library | Glutamine Metabolism Compound Library | NO PAINS Compound Library | Antioxidant Compound Library | Multi-Target Compound Library | Anti-Metabolism Disease Compound Library | Covalent Inhibitor Library |
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网络 第十九章 杂环化合物和生物碱 杂环化合物在自然界分布很广，其数量几乎占已知有机化合物的三分之一，用途也很多。许多重要的物质如叶绿素、血红素、核酸以及临床应用的一些有显著疗效的天然药物和合成药物等，都含有杂环化合物的结构。生物碱多是中草药的有效成分，绝大多数是含氮的杂环化合物。本章内容与医学关系密切，具有重要意义。
分子中具有高能键的化合物。在生物体内主要有上式（Ⅰ）和（Ⅱ）两种结构的高能化合物。其作用为贮藏能量（例如 ATP、肌酸磷酸）和作为产生 ATP源的中间代谢产物（例如磷酸烯醇丙酮酸）以及合成反应的中间物质（例如酰基辅酶 A），在蛋白质的结构（ conformation）变化周期的第一阶段上（例如钠钾 ATP酶的羧基磷酸中间体）也具有重要作用。多数高等化合物具有磷酸基，但也有例外。
由不同种元素组成的纯净物叫做化合物。化合物一般有固定的组成。化合物的组成一般可用化学式表示。化合物具有确定的物理性质和化学性质，不同于其组成元素的性质。化合物中的元素不能用简单的机械方法或物理方法分开，而必须用化学方法才能分离。
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化合物 MPO-IN-28【37836-90-1】
￥194 - 3032
