2-乙酰基吩噻嗪
| 中文名称 | 2-乙酰基吩噻嗪 |
|---|---|
| 中文同义词 | 2-乙酰吩噻嗪;2-乙酰基吩噻嗪;2-乙酰基酚噻嗪;1-(10H-吩噻嗪-2-基)乙酮 |
| 英文名称 | 2-Acetylphenothiazine |
| 英文同义词 | 2-ACETYLPHENOTHIAZINE;methyl phenothiazin-2-yl ketone;2-Acetyl-10H-phenothiazine;2-Acetylphenothiazin;1-(10H-Phenothiazin-2-yl)ethan-1- one, 2-Ethanoyl-10H-phenothiazine;ML 171;LABOTEST-BB LT00012652;NOX1 Inhibitor, ML171 |
| CAS号 | 6631-94-3 |
| 分子式 | C14H11NOS |
| 分子量 | 241.31 |
| EINECS号 | 229-626-4 |
| 相关类别 | 合成;有机杂环;Building Blocks;Heterocyclic Building Blocks;Thiazines;Aromatics;Heterocycles;Inhibitors;Intermediates & Fine Chemicals;Pharmaceuticals |
| Mol文件 | 6631-94-3.mol |
| 结构式 |  |
2-乙酰基吩噻嗪 性质
| 熔点 | 180-185 °C (lit.) |
|---|---|
| 沸点 | 455.7±34.0 °C(Predicted) |
| 密度 | 1.249±0.06 g/cm3(Predicted) |
| 储存条件 | Sealed in dry,2-8°C |
| 溶解度 | 可溶于DMSO（轻微）、甲醇（轻微、加热） |
| 酸度系数(pKa) | -2.45±0.20(Predicted) |
| 形态 | 暗黄橙色粉末 |
| 颜色 | 黄色至深橙色 |
| 最大波长(λmax) | 244nm(MeOH)(lit.) |
| CAS 数据库 | 6631-94-3(CAS DataBase Reference) |
| Target | Value |
|
NOX1
(HEK293) | 0.25 μM |
|
NOX3
(HEK293) | 3 μM |
|
NOX2
(HEK293) | 5 μM |
|
NOX4
(HEK293) | 5 μM |
|
xanthine oxidase
(HEK293) | 5.5 μM |
Nox1-dependent ROS generation has been shown to play a pivotal role in cell signaling, cell growth, angiogenesis, motility and blood pressure regulation. ML171 strongly blocks ROS generation in HT29 cells (IC 50 =0.129 μM) and only increasing over-expression of Nox1 can overcome the blockage of ROS generation caused by ML171 treatment in HEK293 cell system reconstituted with all the components required Nox1-dependent ROS generation. ML171 efficiently blocks ROS production measured by carboxy-H2-DCFDA staining as well as DPI used as a positive control. When ML171 is tested in HEK293-Nox1 reconstituted cell system, higher potency in blocking Nox1-dependent ROS generation is observed compared with the parental compound.
| 提供商 | 语言 |
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英文
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