α-NETA
Based on 13 publication(s) in Google Scholar
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.
For research use only. We do not sell to patients.
- Purity: ≥98.0%
- CAS No.: 115066-04-1
- Formula: C16H20INO
- Molecular Weight:369.24
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) α-NETA
More- Mol Ther. 2025 Oct 6:S1525-0016(25)00830-5. [Abstract]
- Allergy. 2025 Sep 15. [Abstract]
- MedComm (2020). 2024 Aug 31;5(9):e681. [Abstract]
- Acta Biomater. 2024 Apr 15:179:371-384. [Abstract]
- Hypertension. 2024 Apr;81(4):861-875. [Abstract]
- Neural Regen Res. 2024 Sep 6. [Abstract]
- Eur J Pharmacol. 2022 Dec 5:936:175343. [Abstract]
- iScience. 2025 Aug 19;28(9):113396. [Abstract]
- Heliyon. 2024 Apr 9;10(8):e29426. [Abstract]
- BMC Endocr Disord. 2023 Jan 10;23(1):9. [Abstract]
- Eur J Neurosci. 2024 Sep;60(5):4830-4842. [Abstract]
- Blood Press. 2024 Dec;33(1):2414072. [Abstract]
- Research Square Preprint. 2023 Sep 18.
Customer Validation & Images
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ELISA
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Cell Imaging/Staining
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Flow Cytometry
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In Vivo Efficacy Study
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Bio/Physico-chemical Assay
All Chemerin Receptor Isoforms
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Biological Activity
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ALDH1 |
AChE |
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; 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[2].
α-NETA possesses fluorescent characteristics (excitation spectrum: maxima 255 and 297 nm; emission spectrum: maximum 437 nm) of naphthyl moiety[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Ho8910, Ho8910PM, A2780, and Iose80 cells
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Concentration:50, 100, 150 nM
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Incubation Time:24 hours
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Result:Decreased all cell lines viability in a dose-dependent manner.
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Cell Line:Epithelial ovarian cancer (EOC) cell
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Concentration:2.5, 7.5, 10.0 µg/mL
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Incubation Time:24 hours
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Result:Led to EOC cell death associated with membrane blistering and cytoplasm leakage.
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].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude mice with skov3 cells[3]
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Dosage:0.125 mg/kg
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Administration:IP; once every other day for 20 days
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Result:Significantly decreased tumor volume and tumor weight.
Chemical Information
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CAS No. 115066-04-1
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Appearance Solid
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Molecular Weight 369.24
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Formula C16H20INO
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Color White to off-white
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SMILES
O=C(CC[N+](C)(C)C)C1=CC=CC2=C1C=CC=C2.[I-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (13)
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Journal Impact Factor
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Most Recent
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Mol Ther
PAD4 promotes macrophage migration to aggravate tubulointerstitial injury in diabetic kidney disease. [Abstract]2025 Oct 6:S1525-0016(25)00830-5. PMID: 41054305 -
Allergy
Acetylcholine From Solitary Chemosensory Cell, Not Neuron, Regulates Basal Cell Fate Driving Eosinophilic Chronic Rhinosinusitis With Nasal Polyps. [Abstract]2025 Sep 15. PMID: 40951952
α-NETA purchased from MedChemExpress. Usage Cited in: Allergy. 2025 Sep 15. [Abstract]
Histogram showing Ach concentrations in the basolateral medium of ALI cultures under the following conditions: Untreated, α-NETA-treated, and IL-4/IL-5/IL-13 treatment with or without α-NETA (10 μM, basal media was changed every 2 days for 21 days), as measured by ELISA.
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MedComm (2020)
Statins, but not proprotein convertase subtilisin-kexin type 9 inhibitors, lower chemerin in hypercholesterolemia via low-density lipoprotein receptor upregulation. [Abstract]2024 Aug 31;5(9):e681. PMID: 39220103
α-NETA purchased from MedChemExpress. Usage Cited in: MedComm (2020). 2024 Aug 31;5(9):e681. [Abstract]
The CMKLR1 antagonist α-NETA, pravastatin, atorvastatin, rosuvastatin, alirocumab, and evolocumab prevented this effect in the presence of serum, while only α-NETA (3 µmol/L) and pravastatin prevented it in the presence of ApoA-I.
α-NETA purchased from MedChemExpress. Usage Cited in: MedComm (2020). 2024 Aug 31;5(9):e681. [Abstract]
Western blot analysis of cell lysates revealed that α‐NETA (3 µmol/L), either with or without chemerin‐9, upregulated HMGCR, ABCA1, and ABCG1, while a similar tendency was shown for liver X receptors α and β (LXRα and LXRβ).
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Acta Biomater
Vascular stent with immobilized anti-inflammatory chemerin 15 peptides mitigates neointimal hyperplasia and accelerates vascular healing. [Abstract]2024 Apr 15:179:371-384. PMID: 38382829 -
Hypertension
Statins Prevent the Deleterious Consequences of Placental Chemerin Upregulation in Preeclampsia. [Abstract]2024 Apr;81(4):861-875. PMID: 38361240
α-NETA purchased from MedChemExpress. Usage Cited in: Hypertension. 2024 Apr;81(4):861-875. [Abstract]
Chemerin-9 constricted both healthy and preeclamptic chorionic plate arteries although its effects were much smaller (P<0.0001) in the latter. In both groups, pravastatin (20 μmol/L) and the chemerin1/CMKLR1 receptor antagonist α-NETA (3 μmol/L) blocked these constrictor effects. The ET-1-induced constrictor effects were also smaller (P<0.01) in preeclamptic chorionic plate arteries.
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Neural Regen Res
Chemerin 15 peptide reduces neuroinflammation via the ChemR23 receptor after ischemia-reperfusion injury. [Abstract]2024 Sep 6. PMID: 39248165 -
Eur J Pharmacol
Chemerin-9 in paraventricular nucleus increases sympathetic outflow and blood pressure via glutamate receptor-mediated ROS generation. [Abstract]2022 Dec 5:936:175343. PMID: 36306926 -
iScience
Chemerin 15 enhances microglial phagocytosis to attenuate cerebral ischemia-reperfusion injury through the ChemR23/p38 MAPK pathway. [Abstract]2025 Aug 19;28(9):113396. PMID: 40970195
α-NETA purchased from MedChemExpress. Usage Cited in: iScience. 2025 Aug 19;28(9):113396. [Abstract]
α-NETA (100 nM, 24 h), a competitive inhibitor of ChemR23, was used in subsequent experiments. Compared with the OGD+C15 group, the proportion of microglia containing Zymosan and the Zymosan+ area decreased in the α-NETA group, showing no statistical difference from the OGD group.
α-NETA purchased from MedChemExpress. Usage Cited in: iScience. 2025 Aug 19;28(9):113396. [Abstract]
C15 administration downregulated ChemR23 expression, while a slight increase in its expression was observed in the OGD+C15+α-NETA (100 nM, 24 h) group compared with the OGD+C15 group.
α-NETA purchased from MedChemExpress. Usage Cited in: iScience. 2025 Aug 19;28(9):113396. [Abstract]
α-NETA (10 mg/kg) treatment increased HMGB1 levels. Western blot was used to measure the protein expression of HMGB1 after I/R in mice.
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Heliyon
Electroacupuncture ameliorates gastrointestinal dysfunction by modulating DMV cholinergic efferent signals to drive the vagus nerve in p-MCAO rats. [Abstract]2024 Apr 9;10(8):e29426. PMID: 38638995 -
BMC Endocr Disord
α-NETA down-regulates CMKLR1 mRNA expression in ileum and prevents body weight gains collaborating with ERK inhibitor PD98059 in turn to alleviate hepatic steatosis in HFD-induced obese mice but no impact on ileal mucosal integrity and steatohepatitis progression. [Abstract]2023 Jan 10;23(1):9. PMID: 36624417
α-NETA purchased from MedChemExpress. Usage Cited in: BMC Endocr Disord. 2023 Jan 10;23(1):9. [Abstract]
α‑NETA (30 mg/kg; gavage; single daily for 3 weeks) down‑regulates elevated mRNA expressions of CMKLR1 in ileal tissues of wild-type adult C57BL/6 mice (male, 8-10 weeks old, 18-22 g). normal diet group (ND), high-fat diet group (HFD), HFD+α-NETA group (NETA), HFD+PD98059 group (PD) and HFD+α-NETA+PD98059 group (NETA+PD).
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Eur J Neurosci
Chemerin in caudal division of nucleus tractus solitarius increases sympathetic activity and blood pressure. [Abstract]2024 Sep;60(5):4830-4842. PMID: 39044301 -
Blood Press
Endothelin-1- and acetylcholine-mediated effects in human and rat vessels: impact of perivascular adipose tissue, diabetes, angiotensin II, and chemerin. [Abstract]2024 Dec;33(1):2414072. PMID: 39387176 -
Solvent & Solubility
DMSO : 83.33 mg/mL (225.68 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.08 mg/mL (5.63 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (5.63 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (281 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[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. [Content Brief]
[2]. Graham KL, et al. A novel CMKLR1 small molecule antagonist suppresses CNS autoimmune inflammatory disease. PLoS One. 2014 Dec 1;9(12):e112925. [Content Brief]
[3]. Qiao L, et al. α-NETA induces pyroptosis of epithelial ovarian cancer cells through the GSDMD/caspase-4 pathway. FASEB J. 2019 Nov;33(11):12760-12767. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.7083 mL | 13.5413 mL | 27.0827 mL | 67.7066 mL |
| 5 mM | 0.5417 mL | 2.7083 mL | 5.4165 mL | 13.5413 mL | |
| 10 mM | 0.2708 mL | 1.3541 mL | 2.7083 mL | 6.7707 mL | |
| 15 mM | 0.1806 mL | 0.9028 mL | 1.8055 mL | 4.5138 mL | |
| 20 mM | 0.1354 mL | 0.6771 mL | 1.3541 mL | 3.3853 mL | |
| 25 mM | 0.1083 mL | 0.5417 mL | 1.0833 mL | 2.7083 mL | |
| 30 mM | 0.0903 mL | 0.4514 mL | 0.9028 mL | 2.2569 mL | |
| 40 mM | 0.0677 mL | 0.3385 mL | 0.6771 mL | 1.6927 mL | |
| 50 mM | 0.0542 mL | 0.2708 mL | 0.5417 mL | 1.3541 mL | |
| 60 mM | 0.0451 mL | 0.2257 mL | 0.4514 mL | 1.1284 mL | |
| 80 mM | 0.0339 mL | 0.1693 mL | 0.3385 mL | 0.8463 mL | |
| 100 mM | 0.0271 mL | 0.1354 mL | 0.2708 mL | 0.6771 mL |
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