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

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

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CAS No. : 21019-30-7

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Top Publications Citing Use of Products

43 Publications Citing Use of MCE Methyllycaconitine

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

    Methyllycaconitine 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 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 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 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 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 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 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).

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    Description

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

    IC50 & Target[1]

    α7nAChR

     

    Clinical Trial
    Molecular Weight

    682.80

    Formula

    C37H50N2O10
    CAS No.
    SMILES

    CO[C@@H]1[C@@]23[C@@]4([H])[C@](CN([C@]2([H])[C@]([C@H]4OC)([C@@]5([C@]6([H])[C@@]3([H])C[C@@]([C@H](C5)OC)([H])[C@@H]6OC)O)O)CC)(CC1)COC(C7=C(N8C(C[C@@H](C8=O)C)=O)C=CC=C7)=O
    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    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 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 (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. Climbing behavior is scored by an observer who is blind to the drug treatment, and the time spent on climbing the wall (time during which almost two limbs are off the floor) is measured[2].

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

    Methyllycaconitine21019-30-7MLAnAChRNicotinic acetylcholine receptorsamyloid-β peptides-induced cytotoxicitySH-SY5Ymouse striatumAlzheimer’s diseaseInhibitorinhibitorinhibit

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