α-NETA - CAS:115066-04-1

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α-NETA

目录号 : KM6280 CAS No. : 115066-04-1 纯度 : ≥98%

Data Sheet 产品使用指南

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。

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10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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生物活性

α-NETA is a potent and noncompetitive choline acetyltransferase (ChA) inhibitor with an IC₅₀ of 9 μM. α-NETA is a potent ALDH1A1 (IC₅₀=0.04 µM) and chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (ChE; IC₅₀=84 µM) and acetylcholinesterase (AChE; IC₅₀=300 µM). α-NETA has anti-cancer activity.

体外研究

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.

Cell Viability Assay

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

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.

体内研究

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:	BALB/c nude mice with skov3 cells
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

369.24

CAS号

115066-04-1

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

4°C, protect from light, stored under nitrogen

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

溶解性数据

In Vitro:

DMSO : 83.33 mg/mL (225.68 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.7083 mL	13.5413 mL	27.0827 mL
5 mM	0.5417 mL	2.7083 mL	5.4165 mL
10 mM	0.2708 mL	1.3541 mL	2.7083 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 2.08 mg/mL (5.63 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.63 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.08 mg/mL (5.63 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.63 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
3.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 2.08 mg/mL (5.63 mM); Clear solution

此方案可获得 ≥ 2.08 mg/mL (5.63 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。