1. Methyllycaconitine citrate

Methyllycaconitine citrate  (Synonyms: MLA)

Cat. No.: HY-N2332A Purity: 99.03%
COA Handling Instructions

Methyllycaconitine citrate is a specific antagonist of α7 neuronal nicotinic acetylcholine receptor (α7nAChR) with blood-brain barrier permeability.

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

Methyllycaconitine citrate Chemical Structure

Methyllycaconitine citrate Chemical Structure

CAS No. : 351344-10-0

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Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 115 In-stock
Solution
10 mM * 1 mL in DMSO USD 115 In-stock
Solid
5 mg USD 70 In-stock
10 mg USD 120 In-stock
25 mg USD 270 In-stock
50 mg USD 490 In-stock
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Customer Review

Based on 19 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Methyllycaconitine citrate purchased from MedChemExpress. Usage Cited in: Inflamm Res. 2023 Mar 13.  [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.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • Customer Review

    Description

    Methyllycaconitine citrate is a specific antagonist of α7 neuronal nicotinic acetylcholine receptor (α7nAChR) with blood-brain barrier permeability.

    IC50 & Target

    α7nAChR[1]

    In Vitro

    Pretreatment with 5 and 10 μM Methyllycaconitine citrate (MLA) inhibits the decreased cell viability induced by Aβ25-35. Cell viability does not decrease after exposure to Methyllycaconitine citrate (2.5, 5, 10, 20 μM). Aβ25-35 treatment increases LC3-II levels, which is inhibited by administration of Methyllycaconitine citrate. Methyllycaconitine citrate also inhibits Aβ-induced autophagosome accumulation in SH-SY5Y cells. Flow cytometry also demonstrates decreased MDC-labeled vacuoles with Methyllycaconitine citrate treatment[1].

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

    In Vivo

    Methyllycaconitine citrate (MLA) (6 mg/kg) given alone intraperitoneally does not cause climbing behavior when compare with the saline group. Pretreatment with Methyllycaconitine citrate significantly inhibits methamphetamine (METH)-induced climbing behavior, by about 50%. Methyllycaconitine citrate does not modify either basal locomotor activity or METH-induced hyperlocomotion. The METH-induced depletion of dopamine neuron terminals is attenuated in mice pretreated with Methyllycaconitine citrate (250±43 fmol/mg, n=7). A direct effect of Methyllycaconitine citrate on body temperature is ruled out because Methyllycaconitine citrate does not affect basal body temperature (37.0±0.5°C, n=5) or reduce the METH-induced hyperthermia (38.2±0.4°C, n=6, MLA+METH group, n.s. versus METH group)[1].

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

    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 : 125 mg/mL (142.87 mM; Need ultrasonic; 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)

    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%

    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.

    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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    • 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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