2. GPCR/G Protein Metabolic Enzyme/Protease Neuronal Signaling Apoptosis
  3. Chemerin Receptor Aldehyde Dehydrogenase (ALDH) Cholinesterase (ChE) Apoptosis
  4. α-NETA

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.

α-NETA Chemical Structure

α-NETA Chemical Structure

CAS No. : 115066-04-1

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Customer Review

Based on 11 publication(s) in Google Scholar

α-NETA Related Antibodies

Top Publications Citing Use of Products

    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).

    View All Aldehyde Dehydrogenase (ALDH) Isoform Specific Products:

    View All Isoforms
    ALDH1 ALDH2 ALDH3

    View All Cholinesterase (ChE) Isoform Specific Products:

    View All Isoforms
    AChE BChE

    • Biological Activity

    • Purity & Documentation

    • References

    • Customer Review

    Description

    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].

    IC50 & Target

    ALDH1

     

    AChE

     

    In Vitro

    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.

    α-NETA Related Antibodies

    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

    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].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    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.
    Molecular Weight

    369.24

    Formula

    C16H20INO
    CAS No.
    Appearance

    Solid

    Color

    White to off-white

    SMILES

    O=C(CC[N+](C)(C)C)C1=CC=CC2=C1C=CC=C2.[I-]
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, protect from light, stored under nitrogen

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    Solvent & Solubility
    In Vitro: 

    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the 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 (protect from light, stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    • Molarity Calculator

    • Dilution Calculator

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass
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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

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    Volume (start)

    V1

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    Concentration (final)

    C2

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    Volume (final)

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    In Vivo:

    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.

    • Protocol 1

      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.
    • Protocol 2

      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.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    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).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light, stored under nitrogen)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    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

    Purity: ≥98.0%

    SDS (252 KB)

    COA (251 KB) HNMR (254 KB) MS (68 KB)

    Handling Instructions (2659 KB)
    References

    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 (protect from light, stored under nitrogen). 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
    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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    α-NETA Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    α-NETA115066-04-1Chemerin ReceptorAldehyde Dehydrogenase (ALDH)Cholinesterase (ChE)ApoptosisHo8910Ho8910PMA2780Iose80cholineacetyltransferaseCMKLR1cholinesteraseALDH1A1G9ahistonelysinemethyltransferasefluorescentβ-ARR2β-arrestin2Inhibitorinhibitorinhibit

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