Powder: -20°C for 3 years | In solvent: -80°C for 1 year
MPO-IN-28 是髓过氧化物酶 (MPO) 抑制剂,IC50=44 nM。
规格 | 价格/CNY | 货期 | 数量 | |
---|---|---|---|---|
1 mg | ¥ 372 | 现货 | ||
2 mg | ¥ 498 | 现货 | ||
5 mg | ¥ 747 | 现货 | ||
10 mg | ¥ 1,230 | 现货 | ||
25 mg | ¥ 2,080 | 现货 | ||
50 mg | ¥ 3,130 | 现货 | ||
100 mg | ¥ 4,480 | 现货 | ||
200 mg | ¥ 6,330 | 现货 | ||
1 mL * 10 mM (in DMSO) | ¥ 1,320 | 现货 |
产品描述 | MPO-IN-28 is a novel potent, irreversible Myeloperoxidase (MPO) inhibitor with IC50 of 44 nM. |
靶点活性 | MPO:44 nM (cell free) |
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). |
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. |
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). |
分子量 | 231.25 |
分子式 | C11H13N5O |
CAS No. | 37836-90-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 22.73 mg/mL (98.29 mM), Sonication is recommended.
可选溶剂 | 浓度 体积 质量 | 1 mg | 5 mg | 10 mg | 25 mg |
DMSO | 1 mM | 4.3243 mL | 21.6216 mL | 43.2432 mL | 108.1081 mL |
5 mM | 0.8649 mL | 4.3243 mL | 8.6486 mL | 21.6216 mL | |
10 mM | 0.4324 mL | 2.1622 mL | 4.3243 mL | 10.8108 mL | |
20 mM | 0.2162 mL | 1.0811 mL | 2.1622 mL | 5.4054 mL | |
50 mM | 0.0865 mL | 0.4324 mL | 0.8649 mL | 2.1622 mL |
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
MPO-IN-28 37836-90-1 Metabolism Glutathione Peroxidase inhibit Inhibitor MPOIN28 MPO IN 28 inhibitor