Α-NETA
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- CAS号:
- 115066-04-1
- 英文名:
- -NETA
- 英文别名:
- ?-NETA;N2)pyridinato-κ[2-(5-Methyl-1H-pyrazol-3-yl-κ3-2-propenyl)palladium Tetrafluoroborate;3-(Trimethylaminio)-1-(1-naphtyl)-1-propanone;3-(Trimethylaminio)-1-(2-naphtyl)-1-propanone;2-(α-Naphthoyl)ethyltrimethylammonium iodide
- 中文名:
- Α-NETA
- 中文别名:
- 伪-NETA;化合物 Α-NETA;Α-NETA,胆酸酶(CHAT)抑制剂
- CBNumber:
- CB0602624
- 分子式:
- C16H20INO
- 分子量:
- 369.25
- MOL File:
- 115066-04-1.mol
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Α-NETA化学性质
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储存条件:
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−20°C
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形态:
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Solid
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颜色:
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White to off-white
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Α-NETA性质、用途与生产工艺
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。
IC50: 9 μM (ChAT); 0.04 µM (ALDH1A1); CMKLR1; 84 µM (ChE); 300 µM (AChE)
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:
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Ho8910, Ho8910PM, A2780, and Iose80 cells
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Concentration:
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50, 100, 150 nM
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Incubation Time:
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24 hours
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Result:
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Decreased all cell lines viability in a dose-dependent manner.
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Apoptosis Analysis
Cell Line:
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Epithelial ovarian cancer (EOC) cell
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Concentration:
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2.5, 7.5, 10.0 µg/mL
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Incubation Time:
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24 hours
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Result:
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Led to EOC cell death associated with membrane blistering and cytoplasm leakage.
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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:
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BALB/c nude mice with skov3 cells
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Dosage:
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0.125 mg/kg
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Administration:
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IP; once every other day for 20 days
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Result:
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Significantly decreased tumor volume and tumor weight.
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Α-NETA
上下游产品信息
上游原料
下游产品
115066-04-1, Α-NETA 相关搜索:
- C16H20NOI
- 伪-NETA
- Α-NETA,胆酸酶(CHAT)抑制剂
- 化合物 Α-NETA
- 115066-04-1
- N2)pyridinato-&kappa
- 3-2-propenyl)palladium Tetrafluoroborate
- [2-(5-Methyl-1H-pyrazol-3-yl-&kappa
- 3-(Trimethylaminio)-1-(1-naphtyl)-1-propanone
- 3-(Trimethylaminio)-1-(2-naphtyl)-1-propanone
- 2-(α-Naphthoyl)ethyltrimethylammonium iodide
- ?-NETA