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。

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.

Solid

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; IC50=0.04 μM; purified enzymes assay), followed by CMKLR1 (IC50=0.375 μM for β-ARR2 recruitment; Cell-based assay) and G9a histone lysine methyltransferase (IC50=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.

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.
has not independently confirmed the accuracy of these methods. They are for reference only.

Room temperature in continental US; may vary elsewhere.

4°C, protect from light, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

[1]. Sastry BV, et al. Relationships between chemical structure and inhibition of choline acetyltransferase by 2-(alpha-naphthoyl)ethyltrimethylammonium and related compounds. Pharmacol Res Commun. 1988 Sep;20(9):751-71.
[2]. Graham KL, et al. A novel CMKLR1 small molecule antagonist suppresses CNS autoimmune inflammatory disease. PLoS One. 2014 Dec 1;9(12):e112925.

In Vitro: DMSO : 83.33 mg/mL (225.68 mM; Need ultrasonic)配制储备液