生物活性 靶点 体外研究 体内研究
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Α-NETA

Α-NETA,115066-04-1,结构式
Α-NETA
  • CAS号:115066-04-1
  • 英文名:-NETA
  • 中文名:Α-NETA
  • CBNumber:CB0602624
  • 分子式:C16H20INO
  • 分子量:369.25
  • MOL File:115066-04-1.mol
Α-NETA化学性质
  • 储存条件 :−20°C
安全信息

Α-NETA性质、用途与生产工艺

  • 生物活性 α-NETA 是一种有效的,非竞争性的胆碱乙酰转移酶 (ChA) 抑制剂,IC50 为 9 μM。α-NETA 是一种有效的 ALDH1A1 (IC50=0.04 µM) 和趋化因子样受体 1 (CMKLR1) 拮抗剂。α-NETA 微弱的抑制胆碱酯酶 (ChE; IC50=84 µM) 和乙酰胆碱酯 (AChE; IC50=300 µM)。α-NETA 具有抗癌活性。
  • 靶点

    IC50: 9 μM (ChAT); 0.04 µM (ALDH1A1); CMKLR1; 84 µM (ChE); 300 µM (AChE)

  • 体外研究

    α-NETA (50-150 nM; 24 hours) decreases all cell lines viability in a dose-dependent manner.
    α-NETA (2.5-10.0 µg/mL; 24 hours) leads to epithelial ovarian cancer (EOC) cell death associated with membrane blistering and cytoplasm leakage.
    α-NETA treatment increases EOC cell expression of pyroptosis-associated proteins.
    α-NETA is most potent in inhibiting aldehyde dehydrogenase 1 family, member A1 (ALDH1A1; IC 50 =0.04 µM; purified enzymes assay), followed by CMKLR1 (IC 50 =0.375 µM for β-ARR2 recruitment; Cell-based assay) and G9a histone lysine methyltransferase (IC 50 =0.50 µM; purified enzymes assay). α-NETA selectively inhibits chemerin-stimulated CMKLR1 association with β-arrestin2.
    α-NETA possesses fluorescent characteristics (excitation spectrum: maxima 255 and 297 nm; emission spectrum: maximum 437 nm) of naphthyl moiety.

    Cell Viability Assay

    Cell Line: Ho8910, Ho8910PM, A2780, and Iose80 cells
    Concentration: 50, 100, 150 nM
    Incubation Time: 24 hours
    Result: Decreased all cell lines viability in a dose-dependent manner.

    Apoptosis Analysis

    Cell Line: Epithelial ovarian cancer (EOC) cell
    Concentration: 2.5, 7.5, 10.0 µg/mL
    Incubation Time: 24 hours
    Result: Led to EOC cell death associated with membrane blistering and cytoplasm leakage.
  • 体内研究

    α-NETA (i.p.; 0.125 mg/kg; once every other day for 20 days) significantly decreases tumor volume and tumor weight.
    α-NETA (s.c. injection; 3 mg/kg or 10 mg/kg; daily; for 30 days) significantly delays the onset of EAE with 3 mg/kg, and completely suppresses clinical signs for an average of nine days with 10 mg/kg beyond the first appearance of disease in control female C57BL/6 mice.

    Animal Model: BALB/c nude mice with skov3 cells
    Dosage: 0.125 mg/kg
    Administration: IP; once every other day for 20 days
    Result: Significantly decreased tumor volume and tumor weight.
Α-NETA上下游产品信息
上游原料
下游产品
Α-NETA生产厂家
  • 公司名称:TargetMol中国(陶术生物)
  • 联系电话: 4008200310
  • 电子邮件:marketing@tsbiochem.com
  • 国家:中国
  • 产品数:24017
  • 优势度:58
  • 公司名称:美国生物
  • 联系电话:--
  • 电子邮件:sales@advtechind.com
  • 国家:美国
  • 产品数:6106
  • 优势度:58
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