1. GPCR/G Protein Neuronal Signaling Membrane Transporter/Ion Channel
  2. mAChR nAChR
  3. Arecoline

Arecoline, a naturally brain-penetrant and orally active occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline also can induce oxidative stress.

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CAS 番号 : 63-75-2

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Liquid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 33 在庫あり
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10 mM * 1 mL in DMSO USD 33 在庫あり
Liquid
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カスタマーレビュー

Based on 5 publication(s) in Google Scholar

Other Forms of Arecoline:

Top Publications Citing Use of Products

    Arecoline purchased from MedChemExpress. Usage Cited in: Ecotoxicol Environ Saf. 2025 Mar 26:294:118108.  [Abstract]

    Arecoline exhibited a relatively strong binding affinity to PTGS2 in vitro, with a KD value of 10.47 μM.

    Arecoline purchased from MedChemExpress. Usage Cited in: Vet Microbiol. 2025 Dec 15:312:110818.  [Abstract]

    Arecoline (i.p.; single dose) stimulation led to a significant decrease in hepatic and intestinal GSH, SOD, and CAT activities and a significant increase in the MDA content, which were reversed by eFT508 (i.g.; 12 h) administration in BALB/c mice.

    mAChR アイソフォーム固有の製品をすべて表示:

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    製品説明

    Arecoline, a naturally brain-penetrant and orally active occurring psychoactive alkaloid, is a partial agonist of nicotinic and muscarinic acetylcholine receptor. Arecoline exhibits stimulation, alertness, anxiolysis and anti-parasitic effects. Arecoline also can induce oxidative stress[1][2][3][4][5].

    IC50 & Target

    nAChR/mAChR[3]

    Cellular Effect
    Cell Line Type Value Description References
    CHO EC50
    10 3
    Compound: Arecoline
    Stimulation of cAMP in CHO cells expressing human m2 receptor
    Stimulation of cAMP in CHO cells expressing human m2 receptor
    [PMID: 9873644]
    CHO EC50
    10000 1
    Compound: Arecoline
    Stimulation of cAMP in CHO cells expressing human m2 receptor
    Stimulation of cAMP in CHO cells expressing human m2 receptor
    [PMID: 9873644]
    CHO IC50
    115.5 3
    Compound: Arecoline
    Ability to displace [3H]N-methylscopolamine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.
    Ability to displace [3H]N-methylscopolamine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.
    [PMID: 11597415]
    CHO IC50
    0.115 3
    Compound: Arecoline
    Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.
    Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.
    [PMID: 11597415]
    CHO IC50
    115.5 3
    Compound: Arecoline
    Ability to displace [3H]N-methylscopolamine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.
    Ability to displace [3H]N-methylscopolamine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.
    [PMID: 11597415]
    CHO IC50
    0.115 3
    Compound: Arecoline
    Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.
    Ability to displace [3H]oxotremorine from Muscarinic acetylcholine receptor M1 expressed in CHO cells.
    [PMID: 11597415]
    CHO IC50
    145 3
    Compound: arecoline
    Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M1
    Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M1
    [PMID: 9438027]
    CHO IC50
    4.5 3
    Compound: arecoline
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M2
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M2
    [PMID: 9438027]
    CHO IC50
    4.5 3
    Compound: arecoline
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M2
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M2
    [PMID: 9438027]
    CHO IC50
    47.5 3
    Compound: arecoline
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
    [PMID: 9438027]
    CHO IC50
    62.5 3
    Compound: arecoline
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5
    [PMID: 9438027]
    CHO IC50
    47.5 3
    Compound: arecoline
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]-NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M4
    [PMID: 9438027]
    CHO IC50
    58 3
    Compound: arecoline
    Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
    Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
    [PMID: 9438027]
    CHO IC50
    145 3
    Compound: arecoline
    Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M1
    Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M1
    [PMID: 9438027]
    CHO IC50
    62.5 3
    Compound: arecoline
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5
    Compound was evaluated for its ability to displace [3H]- N-methyl-scopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M5
    [PMID: 9438027]
    CHO IC50
    58 3
    Compound: arecoline
    Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
    Compound was evaluated for its ability to displace [3H]N-methylscopolamine ([3H]NMS) binding to cloned CHO cell lines expressing Muscarinic acetylcholine receptor M3
    [PMID: 9438027]
    体外実験

    Arecoline induces the generation of reactive oxygen species and cell cycle arrest at the G1/G0 phase in HaCaT cells without affecting the expression of p21/Cip1. Arecoline-induced epithelial cell death at higher concentrations is caused by oxidative trauma without eliciting apoptosis. Arecoline upregulates the expression of the following stress-responsive genes: hemeoxygenase-1; ferritin light chain; glucose-6-phosphate dehydrogenase; glutamatecysteine ligase catalytic subunit; and glutathione reductase[1].

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

    体内実験

    Arecoline (0.2% in water; p.o., 2 weeks) alleviates the anxiety and depression in CFA (HY-153808)-induced mice[5].

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

    分子量

    155.19

    分子式

    C8H13NO2

    CAS 番号
    Appearance

    Liquid (Density: 1.0495 g/cm3)

    Color

    Light yellow to brown

    SMILES

    O=C(C1=CCCN(C)C1)OC

    Structure Classification
    Initial Source
    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件

    4°C, protect from light

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

    溶剤 & 溶解度
    体外: 

    H2O : 250 mg/mL (1610.93 mM; Need ultrasonic)

    DMSO : 100 mg/mL (644.37 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 6.4437 mL 32.2186 mL 64.4371 mL
    5 mM 1.2887 mL 6.4437 mL 12.8874 mL
    10 mM 0.6444 mL 3.2219 mL 6.4437 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). 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)

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

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始)

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    体内:

    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: ≥ 2.5 mg/mL (16.11 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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: ≥ 2.5 mg/mL (16.11 mM); Clear solution

      This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 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:

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    (per animal)

    g

    Dosing volume
    (per animal)

    μL

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    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
    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).
    純度とドキュメンテーション

    純度: 99.84%

    参考文献

    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). 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 / H2O 1 mM 6.4437 mL 32.2186 mL 64.4371 mL 161.0929 mL
    5 mM 1.2887 mL 6.4437 mL 12.8874 mL 32.2186 mL
    10 mM 0.6444 mL 3.2219 mL 6.4437 mL 16.1093 mL
    15 mM 0.4296 mL 2.1479 mL 4.2958 mL 10.7395 mL
    20 mM 0.3222 mL 1.6109 mL 3.2219 mL 8.0546 mL
    25 mM 0.2577 mL 1.2887 mL 2.5775 mL 6.4437 mL
    30 mM 0.2148 mL 1.0740 mL 2.1479 mL 5.3698 mL
    40 mM 0.1611 mL 0.8055 mL 1.6109 mL 4.0273 mL
    50 mM 0.1289 mL 0.6444 mL 1.2887 mL 3.2219 mL
    60 mM 0.1074 mL 0.5370 mL 1.0740 mL 2.6849 mL
    80 mM 0.0805 mL 0.4027 mL 0.8055 mL 2.0137 mL
    100 mM 0.0644 mL 0.3222 mL 0.6444 mL 1.6109 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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    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    一般には略語で表示されます:C1V1 = C2V2

    濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
    × = ×
    C1   V1   C2   V2
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    製品名:
    Arecoline
    製品番号:
    HY-N2364
    数量:
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