| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg | |||
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| Other Sizes |
| Targets |
α-NETA is a potent inhibitor of choline acetyltransferase (ChAT), the enzyme responsible for the synthesis of acetylcholine. It is also a poor inhibitor of cholinesterases and carnitine acetyltransferase. More recently, it has been identified as a small molecule CMKLR1 antagonist, inhibiting chemerin-stimulated β-arrestin2 association with CMKLR1 with an EC50 of 9.7 nM.
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|---|---|
| ln Vitro |
β-NETA has no effect on cholinesterase, carnitine acetyltransferase, muscarinic receptors, ganglionic nicotinic receptors, or skeletal muscle nicotinic receptors at dosages that inhibit ChA. In guinea pig ileum contractions caused by acetylcholine (ED50=100 µM), histamine, and KCl, β-NETA antagonizes the contraction when the concentration exceeds the IC50 value for inhibiting ChA [2].
In vitro, α-NETA acts as a CMKLR1 antagonist and a choline acetyltransferase inhibitor. Its fluorescent properties make it useful for imaging and tracking in cellular assays. It is commonly used in cell culture studies to investigate cholinergic signaling and CMKLR1-mediated pathways. |
| ln Vivo |
In vivo studies for α-NETA are limited. Its primary use is as a research tool in vitro. However, its activity as a CMKLR1 antagonist suggests potential applications in modulating inflammatory and metabolic pathways in vivo, though these have not been extensively explored.
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| Enzyme Assay |
CMKLR1 antagonism can be assessed using β-arrestin recruitment assays. Cells expressing CMKLR1 and a β-arrestin biosensor are stimulated with chemerin in the presence of varying concentrations of α-NETA. The inhibition of β-arrestin recruitment is measured, and the EC50 is calculated.
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| Cell Assay |
Choline acetyltransferase inhibition is assessed using an in vitro enzyme activity assay. The enzyme is incubated with its substrates, choline and acetyl-CoA, in the presence of varying concentrations of α-NETA. The production of acetylcholine is measured, and the IC50 is calculated.
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| Animal Protocol |
In vivo studies are not typically performed with α-NETA, as it is primarily used as a research tool in vitro. If needed, its effects could be evaluated in animal models of inflammation or metabolic disease by administering the compound and measuring relevant biomarkers.
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| ADME/Pharmacokinetics |
As a small molecule with a molecular weight of 369.2 g/mol, α-NETA is expected to have favorable drug-like properties. It is soluble in methanol or DMSO and sparingly soluble in water. Its pharmacokinetic properties have not been extensively characterized.
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| Toxicity/Toxicokinetics |
Based on its use as a research tool, α-NETA is not typically associated with significant toxicity in vitro at the concentrations used. However, as with any chemical, appropriate safety precautions should be taken when handling it.
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| References |
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| Additional Infomation |
α-NETA is a research compound used as a choline acetyltransferase inhibitor and a CMKLR1 antagonist. Its fluorescent properties make it a versatile tool for studying cholinergic signaling and chemokine receptor pathways in cell culture.
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| Molecular Formula |
C16H20INO
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|---|---|
| Molecular Weight |
369.24
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| Exact Mass |
369.058
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| CAS # |
31059-54-8
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| PubChem CID |
169245
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| Appearance |
White to off-white solid powder
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| LogP |
4.117
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
19
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| Complexity |
292
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LIFHUGCXEAQKRZ-UHFFFAOYSA-M
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| InChi Code |
InChI=1S/C16H20NO.HI/c1-17(2,3)11-10-16(18)15-9-8-13-6-4-5-7-14(13)12-15;/h4-9,12H,10-11H2,1-3H3;1H/q+1;/p-1
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| Chemical Name |
trimethyl-(3-naphthalen-2-yl-3-oxopropyl)azanium;iodide
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| Synonyms |
αNETA; α NETA; α-NETA
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~31.25 mg/mL (~84.63 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (5.63 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (5.63 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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