1. Metabolic Enzyme/Protease
  2. MAGL
  3. MAGLi 432

MAGLi 432 是一种非共价的、有效的、高选择性的、可逆的 (MAGL) 抑制剂。MAGLi 432 以高亲和力结合 MAGL 活性位点,IC50 值为 4.2 nM (human enzyme) 和 3.1 nM (mouse enzyme)。MAGLi 432 可用于慢性炎症、血脑屏障功能障碍、多发性硬化症、阿尔茨海默病和帕金森病等神经系统疾病的研究。

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MAGLi 432 Chemical Structure

MAGLi 432 Chemical Structure

CAS No. : 2361575-20-2

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

MAGLi 432 is a non-covalent, potent, highly selective, and reversible MAGL inhibitor. MAGLi 432 binds with high affinity to the MAGL active site, with IC50 values of 4.2 nM (human enzyme) and 3.1 nM (mouse enzyme). MAGLi 432 can be used in the research of chronic inflammation, blood–brain barrier dysfunction, neurological disorders such as multiple sclerosis, Alzheimer’s disease and Parkinson’s disease[1].

体外研究
(In Vitro)

MAGLi 432 (10 μΜ, 25 min) displays selectivity and potency for MAGL over other serine hydrolases in mouse and human brain lysates[1].
MAGLi 432 (1 μΜ, 6 h) inhibits MAGL activity and robustly enhances 2-AG levels in human NVU cells[1].

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

Western Blot Analysis[1]

Cell Line: Human BMECs (hCMEC/D3), primary human astrocytes, and pericytes
Concentration: 10 nM, 100 nM, 1 μM and 10 μM
Incubation Time: 6 h
Result: Inhibited MAGL activity in a dose-dependent manner, and increased 2-AG levels in all cell types.
Modulated arachidonic acid levels in a cell specific-manner, with no effect in BMECs, but significant depletion in astrocytes and pericytes.
体内研究
(In Vivo)

MAGLi 432 (intraperitoneal injection, 1 mg/kg for 3 consecutive days) inhibits MAGL in the brain and reduces arachidonic acid and PGE2 levels in LPS-induced neuroinflammation, without reducing BBB permeability and inflammatory cytokine expression in the cortex[1].

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

Animal Model: Male CD-1 mice model of LPS-induced neuroinflammation[1]
Dosage: 1 mg/kg for 3 consecutive days
Administration: Intraperitoneal injection
Result: Accumulated ~10-fold more 2-AG than vehicle controls, reducted LPS-induced PGE2.
Increased LCN2 and TNF expression compared to the LPS treatment.
分子量

463.80

Formula

C22H24BrClN2O2

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

MAGLi 432 相关分类

  • 摩尔计算器

  • 稀释计算器

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

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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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MAGLi 432
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HY-150702
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