1. Membrane Transporter/Ion Channel Autophagy Metabolic Enzyme/Protease
  2. P-glycoprotein Autophagy Endogenous Metabolite
  3. Piperine

Piperine  (Synonyms: Bioperine; 1-Piperoylpiperidine)

Cat. No.: HY-N0144 Purity: 98.88%
COA Handling Instructions

Piperine, a natural alkaloid isolated from Piper nigrum L, inhibits P-glycoprotein and CYP3A4 activities with an IC50 value of 61.94±0.054 μg/mL in HeLa cell.

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

Piperine Chemical Structure

Piperine Chemical Structure

CAS No. : 94-62-2

Size Price Stock Quantity
Free Sample (0.1 - 0.5 mg)   Apply Now  
Solid + Solvent
10 mM * 1 mL in DMSO
ready for reconstitution
USD 33 In-stock
Solution
10 mM * 1 mL in DMSO USD 33 In-stock
Solid
5 g USD 30 In-stock
10 g USD 50 In-stock
50 g   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 13 publication(s) in Google Scholar

Other Forms of Piperine:

Top Publications Citing Use of Products

    Piperine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457.   [Abstract]

    Piperine inhibits AMPK activation. HK-2 cells are treated as indicated and the levels of p-AMPK, total AMPK, and β-tubulin are examined by Western blot.

    Piperine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457.   [Abstract]

    Piperine targets NLRP3 inflammasome by blocking AMPK activation. HK-2 cells are treated as indicated.

    Piperine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457.   [Abstract]

    Piperine inhibits the activation of NLRP3 inflammasome. The protein levels of indicated targets are examined by Western blot.

    Piperine purchased from MedChemExpress. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457.   [Abstract]

    Piperine targets NLRP3 inflammasome in HK-2 cells. The protein levels of indicated proteins in cell lysates and from culture medium are examined by Western blot.
    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

    Piperine, a natural alkaloid isolated from Piper nigrum L, inhibits P-glycoprotein and CYP3A4 activities with an IC50 value of 61.94±0.054 μg/mL in HeLa cell.

    IC50 & Target

    IC50: 61.94±0.054 μg/mL (P-glycoprotein, HeLa cell)[1]

    In Vitro

    Piperine has shown to possess in vitro cytotoxic activity and in silico studies. The IC50 value is found to be 61.94±0.054 μg/mL and in silico studies, it has more number of hydrogen bonds with minimum binding and docking energy and may be considered as inhibitor of EGFR tyrosine kinase[1]. Piperine has been found to have immunomodulatory, anti-oxidant, anti-asthmatic, anti-carcinogenic, anti-inflammatory, anti-ulcer, and anti-amoebic properties[2]. Piperine could enhance the bioavailabilities of other drugs including rosuvastatin, peurarin and docetaxel (DOX) via inhibition of CYP3A and P-glycoprotein activity[3].

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

    In Vivo

    At the dose of 3.5 mg/kg, the bioavailability of piperine is calculated to be 25.36%. Its AUC0→t is unproportionally increased with doses, indicating a potential non-linear pharmacokinetics profile of piperine. It is found that the AUC0→t and C0 of Docetaxel (HY-B0011) and t1/2 of piperine are significantly increased after their combination use, suggesting potential enhanced bioavailability of not only Docetaxel but also Piperine, which may lead to the overall enhanced pharmacological effects[3]. The phosphorylation of I-κB, p65, p38, ERK, and JNK is inhibited by piperine in a dose-dependent manner, indicating that piperine may be a potential anti-inflammatory drug both in endometritis and in other S. aureus-induced diseases[4].

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

    Clinical Trial
    Molecular Weight

    285.34

    Formula

    C17H19NO3

    CAS No.
    Appearance

    Solid

    Color

    White to light yellow

    SMILES

    O=C(N1CCCCC1)/C=C/C=C/C2=CC=C(OCO3)C3=C2

    Structure Classification
    Initial Source
    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    Solvent & Solubility
    In Vitro: 

    DMSO : 50 mg/mL (175.23 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 3.5046 mL 17.5230 mL 35.0459 mL
    5 mM 0.7009 mL 3.5046 mL 7.0092 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    • 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: ≥ 2.5 mg/mL (8.76 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 (8.76 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).
    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: 98.88%

    References
    Cell Assay
    [1]

    Standard solution is prepared by dissolving 10 mg of piperine in 100 mL of methanol. The MTT assay is carried out to measure cell viability. Ten thousand cells in 100 μL of DMEM media are seeded in the wells of a 96-well plate. After 24 h, existing media is removed and 100 μL of various concentrations of piperine (20–100 μg/mL) are added and incubated for 48 h at 37 °C in a CO2 incubator. Control cells are supplemented with 0.05 % DMSO vehicle. At the 48th hour of incubation, MTT (10 μL of 5 mg/mL) is added to the plate. The contents of the plate are pipetted out carefully, the formazan crystals formed are dissolved in 100 μL of DMSO, and the absorbance is measured at 550 nm in a microplate reader[1].

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

    Animal Administration
    [3][4]

    Rats: The stock solutions of piperine (PIP) and docetaxel (DOX)are prepared by dissolving appropriate amount of each authentic compound in DMSO separately at 1 mg/mL. The standard solutions containing both PIP and DOX are prepared by serial dilution of the stock solutions with 0.2% formic acid and acetonitrile (50:50, v/v) to yield concentrations of 25, 50, 100, 200, 400, 800, 1600, 3200, 6400, 12800 ng/mL. 25 Sprague-Dawley rats are divided into five groups receiving DOX(Group DOX 7 iv, 7 mg/kg, i.v.), PIP (Group PIP 35 po, 35 mg/kg,p.o.) and their combined administration (Group DOX+PIP) as well as PIP (Group PIP 3.5 po, 3.5 mg/kg, p.o.) and PIP (Group PIP 3.5 iv, 3.5 mg/kg, i.v.)[3].

    Mice: Piperine is dissolved in 5 mL of tris buffered saline (TBS) at concentrations corresponding to 25, 50, and 100 mg/kg, based on the weight of the mice. After 24 h of S. aureus infection in the uterus, the piperine solution is injected intraperitoneally three times every 6 h. A total of 60 female BALB/c mice are used in this study. All mice are maintained on a 12 h light/dark cycle and cafeteria feeding[4].

    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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 3.5046 mL 17.5230 mL 35.0459 mL 87.6148 mL
    5 mM 0.7009 mL 3.5046 mL 7.0092 mL 17.5230 mL
    10 mM 0.3505 mL 1.7523 mL 3.5046 mL 8.7615 mL
    15 mM 0.2336 mL 1.1682 mL 2.3364 mL 5.8410 mL
    20 mM 0.1752 mL 0.8761 mL 1.7523 mL 4.3807 mL
    25 mM 0.1402 mL 0.7009 mL 1.4018 mL 3.5046 mL
    30 mM 0.1168 mL 0.5841 mL 1.1682 mL 2.9205 mL
    40 mM 0.0876 mL 0.4381 mL 0.8761 mL 2.1904 mL
    50 mM 0.0701 mL 0.3505 mL 0.7009 mL 1.7523 mL
    60 mM 0.0584 mL 0.2920 mL 0.5841 mL 1.4602 mL
    80 mM 0.0438 mL 0.2190 mL 0.4381 mL 1.0952 mL
    100 mM 0.0350 mL 0.1752 mL 0.3505 mL 0.8761 mL
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.
    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.

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

     

    Salutation

    Applicant Name *

     

    Email Address *

    Phone Number *

     

    Organization Name *

    Department *

     

    Requested quantity *

    Country or Region *

         

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Piperine
    Cat. No.:
    HY-N0144
    Quantity:
    MCE Japan Authorized Agent: