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  3. α-NETA

α-NETA 

Cat. No.: HY-124957
Handling Instructions

α-NETA is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM. α-NETA is a potent chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM). α-NETA has anti-cancer activity.

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α-NETA Chemical Structure

α-NETA Chemical Structure

CAS No. : 31059-54-8

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Description

α-NETA is a stable, noncompetitive, slowly reversible choline acetyltransferase (ChAT) inhibitor with an IC50 of 9 μM. α-NETA is a potent chemokine-like receptor-1 (CMKLR1) antagonist. α-NETA weakly inhibits cholinesterase (IC50=84 µM) and acetylcholinesterase (IC50=300 µM). α-NETA has anti-cancer activity[1][2].

IC50 & Target

IC50: 9 μM (ChAT); CMKLR1; 84 µM (cholinesterase); 300 µM (acetylcholinesterase)[1][2]

In Vitro

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].
a-NETA treatment increases EOC cell expression of pyroptosis-associated proteins[3].

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.
In Vivo

a-NETA (injected intraperitoneally; 0.125 mg/kg; once every other day for 20 days) significantly decreases tumor volume and tumor weight[3].
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].

Animal Model: BALB/c nude mice with skov3 cells[3]
Dosage: 0.125 mg/kg
Administration: Injected intraperitoneally; once every other day for 20 days
Result: Significantly decreased tumor volume and tumor weight.
Molecular Weight

369.24

Formula

C₁₆H₂₀INO

CAS No.

31059-54-8

SMILES

O=C(C1=CC=C2C=CC=CC2=C1)CC[N+](C)(C)C.[I-]

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Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

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Keywords:

α-NETAApoptosischolineacetyltransferaseChATchemokine-likereceptor-1CMKLR1cholinesteraseacetylcholinesteraseanti-cancerInhibitorinhibitorinhibit

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