1. GPCR/G Protein Neuronal Signaling Metabolic Enzyme/Protease Apoptosis NF-κB Immunology/Inflammation
  2. 5-HT Receptor FAAH Apoptosis Reactive Oxygen Species (ROS)
  3. 5-HT6R/FAAH modulator 1

5-HT6R/FAAH modulator 1 是一种选择性血清素 5-HT6 受体配体和脂肪酸酰胺水解酶 (FAAH) 抑制剂。5-HT6R/FAAH modulator 1 对 5-HT6 的 pKi为 6.33,对 FAAHpIC50 为 6.33。5-HT6R/FAAH modulator 1 对乙酰胆碱酯酶 (AChE) 或丁酰胆碱酯酶 (BChE) (pIC50 = 5.12) 也有轻微抑制作用。5-HT6R/FAAH modulator 1 能够抑制细胞凋亡 (apoptosis) 并降低活性氧 (ROS) 水平。5-HT6R/FAAH modulator 1 可用于神经系统疾病的研究,如阿尔茨海默病 (AD)。

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5-HT6R/FAAH modulator 1

5-HT6R/FAAH modulator 1 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

5-HT6R/FAAH modulator 1 is a selective serotonin 5-HT6 receptor ligand and the fatty acid amide hydrolase (FAAH) enzyme inhibitor. 5-HT6R/FAAH modulator 1 shows a pKi of 6.33 (5-HT6) and a pIC50 valuesof 6.29 (FAAH). 5-HT6R/FAAH modulator 1 also slightly inhibits acetylcholinesterase (AChE) or butyrylcholinesterase (BChE) enzymes (pIC50 = 5.12). 5-HT6R/FAAH modulator 1 can inhibit apoptosis and reduce ROS levels. 5-HT6R/FAAH modulator 1 can be used for the research of neurological disease, such as Alzheimer’s disease (AD)[1].

IC50 & Target[1]

5-HT6 Receptor

6.33 (pKi)

体外研究
(In Vitro)

5-HT6R/FAAH modulator 1 (Compound 23) (0.3-30 μM, 72 h) 可抑制 HepG2 和 SH-SY5Y 细胞的生长[1]
5-HT6R/FAAH modulator 1 (10 μM, 17 h) 可提高 Aβ1-42 处理的 HT-22 细胞的存活率,抑制细胞凋亡并降低活性氧水平[1]
5-HT6R/FAAH modulator 1 (0.03-0.15 μM) 显示出强大的抗氧化活性[1]

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

Cell Viability Assay[1]

Cell Line: HepG2 and SH-SY5Y cells
Concentration: 0.3, 3 and 30 μM
Incubation Time: 72 h
Result: Inhibited the growth of HepG2 cells by 30 % at a concentration of 3 μM.
Inhibited cell proliferation by only 44 % at the highest concentration of 30 μM.
体内研究
(In Vivo)

5-HT6R/FAAH modulator 1 (Compound 23) (0.3-1 mg/kg,腹腔注射) 可逆转 MK-801 诱导的记忆障碍大鼠模型中的记忆障碍[1]

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

Animal Model: MK-801-induced memory impairment rats models[1]
Dosage: 0.3 and 1 mg/kg
Administration: Intraperitoneally injection
Result: Reversed memory deficits at a dose of 1 mg/kg producing a bell-shape effect.
分子量

494.59

Formula

C26H34N6O4

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
  • 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)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (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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产品名称:
5-HT6R/FAAH modulator 1
目录号:
HY-175816
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