-NETA
- Product Name
- -NETA
- CAS No.
- 115066-04-1
- Chemical Name
- -NETA
- Synonyms
- ?-NETA;N2)pyridinato-κ[2-(5-Methyl-1H-pyrazol-3-yl-κ3-2-propenyl)palladium Tetrafluoroborate;3-(Trimethylaminio)-1-(1-naphtyl)-1-propanone;3-(Trimethylaminio)-1-(2-naphtyl)-1-propanone;2-(α-Naphthoyl)ethyltrimethylammonium iodide;N,N,N-trimethyl-3-(naphthalen-1-yl)-3-oxopropan-1-aminium
- CBNumber
- CB0602624
- Molecular Formula
- C16H20INO
- Formula Weight
- 369.25
- MOL File
- 115066-04-1.mol
-NETA Property
- storage temp.
- −20°C
- solubility
- DMSO: 2mg/mL, clear
- form
- Solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- CS-0144860
- Product name
- α-NETA
- Purity
- ≥98.0%
- Packaging
- 5mg
- Price
- $75
- Updated
- 2021/12/16
- Product number
- CS-0144860
- Product name
- α-NETA
- Purity
- ≥98.0%
- Packaging
- 10mg
- Price
- $130
- Updated
- 2021/12/16
- Product number
- CS-0144860
- Product name
- α-NETA
- Purity
- ≥98.0%
- Packaging
- 25mg
- Price
- $250
- Updated
- 2021/12/16
- Product number
- CS-0144860
- Product name
- α-NETA
- Purity
- ≥98.0%
- Packaging
- 50mg
- Price
- $400
- Updated
- 2021/12/16
- Product number
- CS-0144860
- Product name
- α-NETA
- Purity
- ≥98.0%
- Packaging
- 100mg
- Price
- $600
- Updated
- 2021/12/16
-NETA Chemical Properties,Usage,Production
Uses
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[1][2].
Biological Activity
Originally identified as a substrate (ChA or choline)-noncompetitive, slowly reversible choline acetyltransferase inhibitor (human ChAT/BuChE/AChE IC50 = 88 nM/33.3 μM/48.6 μM; does not affect mAChRs, AChE, ChE, CrAT, ganglionic or skeletal muscular nAChRs), α-NETA is a fluorescent molecule (Ex 255 & 297 nm; Em 427 nm) also known for its trace amine-associated receptor 5 (TAAR5 EC50 = 150 nM) agonist and chemokine-like receptor-1 antagonist (IC50 = 375 nM; 7 nM chemerin-induced CMKLR1 β-ARR2 recruitment) potencies both in cultures and in animal disease models in vivo (3-20 mg/kg via ip. or sc. in rats & mice).
in vivo
α-NETA (i.p.; 0.125 mg/kg; once every other day for 20 days) significantly decreases tumor volume and tumor weight[3].
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].
| Animal Model: | BALB/c nude mice with skov3 cells[3] |
| Dosage: | 0.125 mg/kg |
| Administration: | IP; once every other day for 20 days |
| Result: | Significantly decreased tumor volume and tumor weight. |
IC 50
ALDH1; AChE
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. DOI:10.1016/s0031-6989(88)80715-x
[2] Graham KL, et al. A novel CMKLR1 small molecule antagonist suppresses CNS autoimmune inflammatory disease. PLoS One. 2014 Dec 1;9(12):e112925. DOI:10.1371/journal.pone.0112925
[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. DOI:10.1096/fj.201900483RR
-NETA Preparation Products And Raw materials
Raw materials
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