2. Apoptosis Metabolic Enzyme/Protease Neuronal Signaling NF-κB Immunology/Inflammation
  3. Glutathione Peroxidase Ferroptosis Monoamine Oxidase Reactive Oxygen Species (ROS) Tau Protein Amyloid-β
  4. MAO-B-IN-45

MAO-B-IN-45 是一种铁死亡 (ferroptosis) 和 MAO-B 的双重抑制剂。MAO-B-IN-45 对 MAO-B 具有选择性，IC50 为 87.47 nM，对 MAO-B 的选择性比 MAO-A 高 229 倍以上。MAO-B-IN-45 在体外通过调节铁代谢途径和 GSH-GPX4 轴表现出卓越的抗铁死亡活性。MAO-B-IN-45 能改善 3×Tg (APP/Tau/Ps1) 阿尔茨海默病小鼠的认知和行为障碍，并显著降低其脑内铁蛋白重链 1 (FTH1)、β-淀粉样蛋白 (APP) 和 Tau 蛋白磷酸化 (p-Tau) 的水平。

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MAO-B-IN-45 Chemical Structure

MAO-B-IN-45 Chemical Structure

CAS No. : 3069915-36-9

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MAO-B-IN-45 相关抗体

Top Publications Citing Use of Products

查看 Monoamine Oxidase 亚型特异性产品:

查看所有亚型
MAO-A MAO-B

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MAO-B-IN-45 is a dual inhibitors of ferroptosis and MAO-B. MAO-B-IN-45 shows selectivity towards MAO-B with an IC50 of 87.47 nM and selectivity exceeding 229-fold for MAO-B over MAO-A. MAO-B-IN-45 has excellent antiferroptosis activity through modulation of the iron metabolic pathway and GSH-GPX4 axis in vitro. MAO-B-IN-45 improves cognitive and behavioral impairments in 3×Tg (APP/Tau/Ps1) AD mouse and significantly reduced the levels of ferritin heavy chain 1 (FTH1), APP, and Tau phosphorylation (p-Tau) proteins in the brain[1].

体外研究
(In Vitro)

MAO-B-IN-45 (compound 21d) 是一种可逆的 hMAO-B 抑制剂，抑制常数 Ki 值为 100.6 nM, 表现出较高的 hMAO-B 抑制活性，抑制率分别为 94.81% (10 μM) 和 76.31% (1 μM)[1]。

MAO-B-IN-45 (0.1-75 μM, 24 h) 在 PC12 细胞和 HT22 细胞中显示出良好的安全性[1]。

MAO-B-IN-45 (1-50 μM, 24 h) 在 HT22 细胞中以剂量依赖的方式有效减轻 RSL (HY-100218A) 或 Erastin (HY-15763) 诱导的铁死亡[1]。

MAO-B-IN-45 (10-50 μM, 24 h) 可降低 HT22 细胞内活性氧 (ROS) 的产生[1]。

MAO-B-IN-45 (15-100 μM, 24 h) 通过减少 HT22 细胞内铁积累和增强谷胱甘肽 (GSH) 依赖途径，有效地抑制铁死亡[1]。

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

MAO-B-IN-45 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: HT22 cells, PC12 cells
Concentration: 25, 50, and 75 μM (HT22 cells), 0.1, 1, 10, 20, 30, 40, 50, 75 μM (PC12 cells)
Incubation Time: 24 h
Result: Showed favorable safety, maintaining a cell viability of 83.56% on PC12 cells and 86.47% on HT22 cells at the highest test concentration (75 μM), warranting further investigation.

Cell Cytotoxicity Assay[1]

Cell Line: RSL3/Erastin-induced HT22 cells
Concentration: 1, 5, 10, 25, 50 μM
Incubation Time: 24 h
Result: Reduced ferroptosis induced by RSL3 and Erastin at a concentration of 10 μM and completely restored cell viability to normal levels at 50 μM.
体内研究
(In Vivo)

MAO-B-IN-45 (Compound 21d) (10 mg/kg, i.p., daily for 35 days) 减轻 3×Tg (APP/Tau/Ps1) 阿尔茨海默病小鼠模型的记忆和认知功能障碍，并在体内显示出良好的安全性[1]。

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

Animal Model: Triple-transgenic (APP/Tau/Ps1) mice (30-35 g, 7 months)[1].
Dosage: 10 mg/kg
Administration: Intraperitoneal injection daily for 35 days
Result: Increased the number of entries, and reduced the latency and distance to the platform, showing effects comparable to those observed in the safinamide and donepezil groups.
Not markedly different from wild-type mice in cognitive function.
No abnormalities in the tissues (heart, liver, spleen, lung, kidney) compared to those of wild type mice (H&E staining).
Normalized FTH1 levels in 3×Tg mice, and significantly increased the expression level of GPX4.
Reduced the protein level of APP, and decreased the site-specificity in p-Tau at Ser202/Thr205.
分子量

315.75

Formula

C17H14ClNO3
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

MAO-B-IN-45 相关分类

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  • 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.

Keywords:

MAO-B-IN-453069915-36-9Glutathione PeroxidaseFerroptosisMonoamine OxidaseReactive Oxygen Species (ROS)Tau ProteinAmyloid-βMAOβ-amyloid peptideAβAbetaAlzheimer’s disease (AD)Monoamine oxidase B (MAO-B)GSH-GPX4ROSInhibitorinhibitorinhibit

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