1. Membrane Transporter/Ion Channel Neuronal Signaling
  2. nAChR
  3. Methyllycaconitine citrate

Methyllycaconitine citrate  (Synonyms: MLA citrate)

Cat. No.: HY-N2332A Purity: 98.88%
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Methyllycaconitine (MLA) citrate is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine citrate alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine citrate prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine citrate can be used for neurological disease research, such as Alzheimer’s disease .

For research use only. We do not sell to patients.

CAS No. : 351344-10-0

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
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Customer Review

Based on 43 publication(s) in Google Scholar

Other Forms of Methyllycaconitine citrate:

Top Publications Citing Use of Products

43 Publications Citing Use of MCE Methyllycaconitine citrate

In Vivo Imaging
WB
RT-PCR
Histological Imaging/Staining
In Vivo Efficacy Study

    Methyllycaconitine citrate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug 14:e00945.  [Abstract]

    3D reconstruction of micro-CT scanned images of the mouse alveolar bone. GTS-21 or MLA were administered in combination with EA in the LIP + SD + EA group, GTS-21 inhibited the progression of bone resorption, whereas Methyllycaconitine (MLA; 6 mg/kg; i.p. daily for 7 d) exacerbated it.

    Methyllycaconitine citrate purchased from MedChemExpress. Usage Cited in: Adv Sci (Weinh). 2025 Aug 14:e00945.  [Abstract]

    Mouse periodontal tissues mRNA expression of pro-inflammatory-related genes IL-1β), IL-6, TNF-α, and anti-inflammatory-related gene IL-10. LIP+SD (LIP with sleep deprivation); EA (10 Hz, 1 mA, square wave) ; GTS-21 (4 mg/kg; i.p. daily for 7 d); Methyllycaconitine (MLA; 6 mg/kg; i.p. daily for 7 d).

    Methyllycaconitine citrate purchased from MedChemExpress. Usage Cited in: Diabetologia. 2025 Dec 15.  [Abstract]

    Immunoblot analysis of α7nAChR after co-IP with an anti-VDAC1 antibody in HTR8/SVneo cells treated with NG (Normal glucose), HG (High glucose), HG + PNU-282987 or HG + MLA (Methyllycaconitine; 24 h).

    Methyllycaconitine citrate purchased from MedChemExpress. Usage Cited in: Acta Pharmacol Sin. 2024 Jul;45(7):1349-1365.  [Abstract]

    TTC staining and quantification showing the blockade of VNS-induced reduction in infarct volume in the MLA (Methyllycaconitine; 2.5 mg/kg; i.p. 1 h before tMCAO model)-treated mice subjected to tMCAO model. Scale bar: 1.0 cm, n = 6.

    Methyllycaconitine citrate purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Apr;72(4):879-892.  [Abstract]

    PNU-282987 (3 mg/kg; i.p.; single daily for consecutively 28 days) signifcantly decreases the expression levels of collagen I, collagen III, and α-SMA in myocardial infarction (MI) rats model, while Methyllycaconitine citrate (MLA; 3 mg/kg; i.p.; single daily for consecutively 28 days) increases these proteins levels.

    Methyllycaconitine citrate purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2021 Dec 17;18(1):291.  [Abstract]

    Immunofluorescence staining of hippocampal sections in each group rats (IL-1β). The microglia transform from ameboid form (α7nAchR(−/−) + taVNS group and Hi MLA  (Methyllycaconitine; (80 μg/kg; 1-week continuous unilaterally local infusions)) + taVNS group) to ramified state (Hi saline + taVNS). Compared with α7nAchR(−/−) + taVNS group and Hi MLA + taVNS group, the co-expression between pro-inflammatory cytokine IL-1β (green) and microglia (red) decreased in Hi saline + taVNS group. IL-1β (green), Iba-1 (red), DAPI (blue), Merge (yellow).

    Methyllycaconitine citrate purchased from MedChemExpress. Usage Cited in: J Neuroinflammation. 2021 Dec 17;18(1):291.  [Abstract]

    The effect of α7nAchR in the hippocampus on the body mass and behavioral experiments of CUMS rats intervened by taVNS at different time points. MLA (Methyllycaconitine; 80 μg/kg; 1-week continuous unilaterally local infusions); taVNS (transcutaneous auricular vagus nerve stimulation).
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Methyllycaconitine (MLA) citrate is a potent, selective, CNS-penetrant, competitive α7nAChR antagonist. Methyllycaconitine citrate alleviates amyloid-β peptides-induced cytotoxicity in SH-SY5Y cells. Methyllycaconitine citrate prevents methamphetamine-induced effects in mouse striatum. Methyllycaconitine citrate can be used for neurological disease research, such as Alzheimer’s disease [1][2][3].

    IC50 & Target[1]

    α7nAChR

     

    Molecular Weight

    874.92

    Formula

    C43H58N2O17

    CAS No.
    Appearance

    Solid

    Color

    White to yellow

    SMILES

    CO[C@@H]1C(C(N(CC)C2)C3(O)[C@H]4OC)([C@@](C[C@@]5([H])[C@@H]6OC)([H])[C@@]6([H])[C@@]3(C[C@@H]5OC)O)[C@@]4([H])[C@@]2(COC(C7=C(N(C8=O)C(C[C@@H]8C)=O)C=CC=C7)=O)CC1.O=C(CC(C(O)=O)(O)CC(O)=O)O

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 100 mg/mL (114.30 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 2.18 mg/mL (2.49 mM; Need ultrasonic and warming)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1430 mL 5.7148 mL 11.4296 mL
    5 mM 0.2286 mL 1.1430 mL 2.2859 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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 (2.38 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 (2.38 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 (sealed storage, away from moisture)

    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: 99.58%

    References
    Cell Assay
    [1]

    Cells are plated in 96-well plates containing complete medium and cultured for 24 h. Then cells are treated with Methyllycaconitine citrate at the indicated concentrations for specified times. After drug treatment, cell viability is measured by MTT assay. Briefly, 10 µL of the MTT solution (5 mg/mL) is added to each well and incubated for 4 h at 37°C. After removing the supernatant, 100 µL DMSO is added into each well. The absorbance is measured at 570 nm with a microplate reader. All experiments are repeated 3 times[1].

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

    Animal Administration
    [2]

    Adult male Swiss CD-1 mice are used in all experiments. They are housed at 22±1°C under a 12-h light/dark cycle with free access to food and drinking water. Climbing behavior is measured. Briefly, mice of 20 to 26 g are intraperitoneally administered saline (5 mL/kg) or Methyllycaconitine citrate (MLA) (6 mL/kg) at the beginning of the test. Twenty minutes later, the animals receive a single dose of saline or methamphetamine (METH) (1 mL/kg) subcutaneously and are placed individually, for habituation, into the experimental chamber consisting of a cylindrical cage with the wall made of plastic bars and covered with a lid. After a 20-min period of exploratory activity, stereotypy measurement is performed for a period of 30 min[2].

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

    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 (sealed storage, away from moisture). 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
    H2O / DMSO 1 mM 1.1430 mL 5.7148 mL 11.4296 mL 28.5740 mL
    DMSO 5 mM 0.2286 mL 1.1430 mL 2.2859 mL 5.7148 mL
    10 mM 0.1143 mL 0.5715 mL 1.1430 mL 2.8574 mL
    15 mM 0.0762 mL 0.3810 mL 0.7620 mL 1.9049 mL
    20 mM 0.0571 mL 0.2857 mL 0.5715 mL 1.4287 mL
    25 mM 0.0457 mL 0.2286 mL 0.4572 mL 1.1430 mL
    30 mM 0.0381 mL 0.1905 mL 0.3810 mL 0.9525 mL
    40 mM 0.0286 mL 0.1429 mL 0.2857 mL 0.7144 mL
    50 mM 0.0229 mL 0.1143 mL 0.2286 mL 0.5715 mL
    60 mM 0.0190 mL 0.0952 mL 0.1905 mL 0.4762 mL
    80 mM 0.0143 mL 0.0714 mL 0.1429 mL 0.3572 mL
    100 mM 0.0114 mL 0.0571 mL 0.1143 mL 0.2857 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    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.

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