| Identification | Back Directory | [Name]
-NETA | [CAS]
115066-04-1 | [Synonyms]
?-NETA
N2)pyridinato-&kappa
[2-(5-Methyl-1H-pyrazol-3-yl-&kappa
3-2-propenyl)palladium Tetrafluoroborate
2-(α-Naphthoyl)ethyltrimethylammonium iodide
3-(Trimethylaminio)-1-(2-naphtyl)-1-propanone
3-(Trimethylaminio)-1-(1-naphtyl)-1-propanone | [Molecular Formula]
C16H20INO | [MDL Number]
MFCD00209857 | [MOL File]
115066-04-1.mol | [Molecular Weight]
369.25 |
| Hazard Information | Back Directory | [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)-noncompetitiveslowly reversible choline acetyltransferase inhibitor (human ChAT/BuChE/AChE IC50 = 88 nM/33.3 μM/48.6 μM; does not affect mAChRsAChEChECrATganglionic 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.
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| [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 |
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| Company Name: |
G-CLONE
|
| Tel: |
400-910-1997 15330005590 |
| Website: |
http://www.g-clone.com/ |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
| Company Name: |
MedChemExpress
|
| Tel: |
021-58955995 |
| Website: |
www.medchemexpress.com |
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