2. Induced Disease Models Products GPCR/G Protein Neuronal Signaling
  3. Nervous System Disease Models mAChR
  4. Epilepsy Models
  5. Pilocarpine

Pilocarpine is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.

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

CAS No. : 92-13-7

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Customer Review

Based on 41 publication(s) in Google Scholar

Other Forms of Pilocarpine:

Pilocarpine Related Antibodies

Top Publications Citing Use of Products

41 Publications Citing Use of MCE Pilocarpine

In Vivo Efficacy Study
Histological Imaging/Staining
WB
IHC
IF

    Pilocarpine purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2025 May 5;23(1):332.  [Abstract]

    Seizure scores across different groups of the Pilocarpine (300 mg/kg; i.p.)-induced SE model.

    Pilocarpine purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2025 May 5;23(1):332.  [Abstract]

    Survival rate analysis among groups of the Pilocarpine (300 mg/kg; i.p.)-induced SE model.

    Pilocarpine purchased from MedChemExpress. Usage Cited in: J Nanobiotechnology. 2025 May 5;23(1):332.  [Abstract]

    Immunofluorescence staining of CD86 (pro-inflammatory) and CD206 (anti-inflammatory) expression in microglia within the hippocampus across groups of the Pilocarpine (300 mg/kg; i.p.)-induced SE model.

    Pilocarpine purchased from MedChemExpress. Usage Cited in: Cells. 2024 Oct 1;13(19):1635.  [Abstract]

    Mice were intravenously injected with Evans blue or sulfonyl-NHS-biotin tracer, followed by intraperitoneal injection of scopolamine, and finally Pilo (300 mg/kg, ip, single dose) was injected to induce epileptic seizures, with close monitoring. The results indicated increased blood-brain barrier permeability in this Pilo-induced epilepsy model.

    Pilocarpine purchased from MedChemExpress. Usage Cited in: Cells. 2024 Oct 1;13(19):1635.  [Abstract]

    Mice were intravenously injected with Evans blue or sulfonyl-NHS-biotin tracer, followed by intraperitoneal injection of scopolamine, and finally Pilo (300 mg/kg, ip, single dose) was injected to induce epileptic seizures, with close monitoring. The results indicated increased blood-brain barrier permeability in this Pilo-induced epilepsy model.

    Pilocarpine purchased from MedChemExpress. Usage Cited in: Cells. 2024 Oct 1;13(19):1635.  [Abstract]

    Mice were intravenously injected with Evans blue or sulfonyl-NHS-biotin tracer, followed by intraperitoneal injection of scopolamine, and finally Pilo (300 mg/kg, ip, single dose) was injected to induce epileptic seizures, with close monitoring. The results indicated increased blood-brain barrier permeability in this Pilo-induced epilepsy model.

    Pilocarpine purchased from MedChemExpress. Usage Cited in: Cell Rep. 2023 Apr 30;42(5):112456.  [Abstract]

    Latency before the first seizure of PTZ and Pilocarpine ((300 mg/kg; i.p.)-induced seizure tests in RACK1 fl/fl or RACK1 cKO mice.

    Pilocarpine purchased from MedChemExpress. Usage Cited in: Immunity. 2022 Aug 9;55(8):1466-1482.e9.  [Abstract]

    The effects of tamoxifen treatment and microglial PDGFB ablation on pilocarpine (100 mg/kg, ip, once every 20 minutes)-induced epilepsy were investigated by implanting telemetry probes into PDGFBNull-MG mice and analyzing their heart rate (HR) and heart rate variability (HRV) before and 3 or 5 weeks after tamoxifen treatment.

    Pilocarpine purchased from MedChemExpress. Usage Cited in: Prog Neurobiol. 2022 Oct:217:102335.  [Abstract]

    The percentages of Foxp3+ Tregs among CD4+ T cells significantly increased in the hippocampal parenchyma of Pilocarpine(280-300 mg/kg; i.p.)-induced SE mice compared with those in the control group.

    Pilocarpine purchased from MedChemExpress. Usage Cited in: Prog Neurobiol. 2022 Oct:217:102335.  [Abstract]

    GFAP immunostaining in the CA1, CA3, and DG regions of the hippocampi of vehicle-treated control mice, PC61-treated control mice, vehicle-treated Pilocarpine (280-300 mg/kg; i.p.) mice, and PC61-treated Pilocarpine mice.

    Pilocarpine purchased from MedChemExpress. Usage Cited in: Cell Mol Neurobiol. 2022 Apr;42(3):777-790.  [Abstract]

    Pilocarpine (325 mg/kg, ip, single dose)-induced status epilepticus (SE) reduced the level of ALOXE3 protein in the hippocampus of mice, but did not reduce it in the temporal lobe cortex.

    Pilocarpine purchased from MedChemExpress. Usage Cited in: Cell Mol Neurobiol. 2022 Apr;42(3):777-790.  [Abstract]

    Pilocarpine (325 mg/kg, ip, single dose)-induced status epilepticus (SE) increases AA levels in the hippocampus of mice.

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    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Pilocarpine is a selective M3-type muscarinic acetylcholine receptor (M3 muscarinic receptor) agonist.

    IC50 & Target

    mAChR3

     

    Cellular Effect
    Cell Line Type Value Description References
    CHO EC50
    63000 nM
    Compound: Pilocarpine
    Stimulation of cAMP in CHO cells expressing human m2 receptor
    Stimulation of cAMP in CHO cells expressing human m2 receptor
    		[PMID: 9873644]
    HEK293 EC50
    0.0175 μM
    Compound: Pilocarpine
    Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
    Agonist activity at human m1 muscarinic acetylcholine receptor expressed in HEK293 cells assessed as calcium mobilization by FLIPR assay
    		[PMID: 25765911]
    In Vitro

    To evaluate the cytotoxicity of Pilocarpine, the morphology and viability of human corneal stromal (HCS) cells are examined by light microscopy and MTT assay, respectively. Morphological observations show that HCS cells exposed to Pilocarpine at a concentration from 0.625 to 20 g/L exhibit dose- and time-dependent proliferation retardation and morphological abnormality such as cellular shrinkage, cytoplasmic vacuolation, detachment from culture matrix, and eventually death, while no obvious difference is observed between those exposed to Pilocarpine below the concentration of 0.625 g/L and controls. Results of MTT assay reveal that the cell viability of HCS cells decrease with time and concentration after exposing to Pilocarpine above the concentration of 0.625 g/L (P<0.01 or 0.05), while that of HCS cells treated with Pilocarpine below the concentration of 0.625 g/L show no significant difference to controls[2]. The partial muscarinic agonist, Pilocarpine, evokes concentration-dependent relaxation with an EC50 of 2.4 mM in isolated segments of rat tail artery that were constricted with Penylephrine (10 to 200 nM)[3].

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

    Pilocarpine Related Antibodies
    In Vivo

    Note:
    Please do not refer to only one article to determine the experimental conditions. It is recommended to determine the optimal experimental conditions (animal strain, age, dosage, frequency and cycle, detection time and indicators, etc.) through preliminary experiments before the formal experiment.

    The Pilocarpine-induced saliva secretion of the control rats (CN) and exercised (EX) rats is examined. A significantly greater amount of saliva is induced by Pilocarpine in the EX rats than in the CN rats (P<0.01). Conversely, the Na+ concentration in the saliva of the EX rats is significantly lower than that of the CN rats (P<0.05)[1].

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

    208.26

    Formula

    C11H16N2O2
    CAS No.
    Appearance

    <34°C Solid,>34°C Liquid

    Color

    Colorless to light yellow

    SMILES

    O=C1OC[C@H](CC2=CN=CN2C)[C@@H]1CC
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    -20°C, protect from light

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

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (480.17 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 4.8017 mL 24.0085 mL 48.0169 mL
    5 mM 0.9603 mL 4.8017 mL 9.6034 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.

    • Molarity Calculator

    • Dilution Calculator

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

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

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    Volume (start)

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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: ≥ 2.5 mg/mL (12.00 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 (12.00 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:

    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)

    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: 99.89%

    SDS (584 KB)

    COA (253 KB) HNMR (139 KB) RP-HPLC (168 KB) LCMS (385 KB)

    Handling Instructions (2659 KB)
    References
    Cell Assay
    [2]

    Cell viability is determined by MTT assay. Briefly, HCS cells are inoculated into a 96-well culture plate (Nunc) at a density of 1×104 cells/100 µL/well, and are cultured and treated. At a 4h interval, the Pilocarpine (0.625 to 20 g/L)-containing medium is replaced entirely with 100 µL serum-free DMEM/F12 medium containing 1.0 g/L MTT, and the cells are incubated at 37°C in the dark for 4h. After the MTT-containing medium is discarded with caution, 150 µL DMSO is added to dissolve the produced formazan crystals at 37°C in the dark for 15 min, and the absorbance at 490 nm is measured with a Multiskan GO microplate reader[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [1]

    Rats[1]
    Male, 10-week-old Wistar rats are assigned to one of two groups, exercise (EX, n=6) and control (CN, n=6). The EX rats are kept for 40 days in cages with a running wheel (SN-451), allowing them to undertake voluntary exercise, while the CN rats are kept in cages with the running wheel locked. On the 40th day, Pilocarpine-induced saliva is measured as follows. Briefly, the rats are anesthetized, preweighed cotton was placed in their mouths sublingually, and Pilocarpine (0.5 mg/kg) is intraperitoneally injected to induce saliva secretion. Each cotton ball is then changed every 10 min for 1 h. The collected cotton balls are weighed again, and the mass of saliva secreted is calculated by subtracting the initial from the final weight.

    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 (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 1 mM 4.8017 mL 24.0085 mL 48.0169 mL 120.0423 mL
    5 mM 0.9603 mL 4.8017 mL 9.6034 mL 24.0085 mL
    10 mM 0.4802 mL 2.4008 mL 4.8017 mL 12.0042 mL
    15 mM 0.3201 mL 1.6006 mL 3.2011 mL 8.0028 mL
    20 mM 0.2401 mL 1.2004 mL 2.4008 mL 6.0021 mL
    25 mM 0.1921 mL 0.9603 mL 1.9207 mL 4.8017 mL
    30 mM 0.1601 mL 0.8003 mL 1.6006 mL 4.0014 mL
    40 mM 0.1200 mL 0.6002 mL 1.2004 mL 3.0011 mL
    50 mM 0.0960 mL 0.4802 mL 0.9603 mL 2.4008 mL
    60 mM 0.0800 mL 0.4001 mL 0.8003 mL 2.0007 mL
    80 mM 0.0600 mL 0.3001 mL 0.6002 mL 1.5005 mL
    100 mM 0.0480 mL 0.2401 mL 0.4802 mL 1.2004 mL
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    Pilocarpine 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:

    Pilocarpine92-13-7mAChRMuscarinic acetylcholine receptorInhibitorinhibitorinhibit

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