β-NETA 是胆碱乙酰转移酶 (ChA;IC50=76 μM) 和胆碱酯酶 (ChE;IC50=40 μM)的非竞争性抑制剂,对乙酰胆碱酯的作用微弱 (AChE;IC50=1 mM)。
产品描述
α-NETA is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM and is a potent chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA has anti-cancer activity[1][2]. α-NETA weakly inhibits cholinesterase (IC50=84 μM) and acetylcholinesterase (IC50=300 μM).
体外活性
a-NETA treatment increases EOC cell expression of pyroptosis-associated proteins[3]. a-NETA (50-150 nM; 24 hours) decreases all cell lines viability in a dose-dependent manner [3]. a-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].
体内活性
a-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]. a-NETA (injected intraperitoneally; 0.125 mg/kg; once every other day for 20 days) significantly decreases tumor volume and tumor weight[3].
Cas No.
31059-54-8
分子式
C16H20INO
分子量
369.24
别名
α-NETA
储存和溶解度
DMSO:31.25 mg/mL (84.63 mM),Need ultrasonic
Powder: -20°C for 3 years
In solvent: -80°C for 2 years