化合物 α-NETA T61454

Product Introduction
Bioactivity


英文名: α-NETA

描述: 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。

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.

存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year

化合物 α-NETA T61454信息由TargetMol中国为您提供，如您想了解更多关于化合物 α-NETA T61454报价、型号、参数等信息，欢迎来电或留言咨询。

注：该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案，不可用于临床诊断或治疗等相关用途