Powder: -20°C for 3 years | In solvent: -80°C for 1 year
α-NETA是一种有效的胆碱乙酰转移酶(ChA)非竞争性抑制剂,IC50值为9μM。同时,它也是ALDH1A1(IC50=0.04μM)和趋化因子样受体1(CMKLR1)的有效拮抗剂。此外,α-NETA对胆碱酯酶(ChE; IC50=84μM)和乙酰胆碱酯酶(AChE; IC50=300μM)的抑制作用较弱。α-NETA亦显示出抗癌活性。
产品描述 | α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC 50 of 9 μM. α-NETA is a potent ALDH1A1 ( IC 50 =0.04 μM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC 50 =84 μM) and acetylcholinesterase (AChE; IC 50 =300 μM). α-NETA has anti-cancer activity [1] [2]. |
体外活性 | α-NETA (50-150 nM; 24 hours) decreases all cell lines viability in a dose-dependent manner [3]. 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 [3]. α-NETA treatment increases EOC cell expression of pyroptosis-associated proteins [3]. 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 [2]. α-NETA possesses fluorescent characteristics (excitation spectrum: maxima 255 and 297 nm; emission spectrum: maximum 437 nm) of naphthyl moiety [1]. Cell Viability Assay [3] 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 [3] 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. |
体内活性 | α-NETA (i.p.; 0.125 mg/kg; once every other day for 20 days) significantly decreases tumor volume and tumor weight [3]. 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 [2]. Animal Model: BALB/c nude mice with skov3 cells [3] Dosage: 0.125 mg/kg Administration: IP; once every other day for 20 days Result: Significantly decreased tumor volume and tumor weight. |
分子量 | 369.246 |
分子式 | C16H20INO |
CAS No. | 115066-04-1 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
对于不同动物的给药剂量换算,您也可以参考 更多...
请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法: 比如您的给药剂量是10 mg/kg,每只动物体重20 g,给药体积100 μL,一共给药动物10 只,您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。
母液配置方法:2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:取 50 μL DMSO 主液,加入 300 μL PEG300, 混匀澄清,再加 50 μL Tween 80,混匀澄清,再加 600 μL ddH2O, 混匀澄清。
您可能有的问题的答案可以在抑制剂处理说明中找到,包括如何准备库存溶液,如何存储产品,以及基于细胞的分析和动物实验需要特别注意的问题。
α-NETA 115066-04-1 Inhibitor inhibitor inhibit