1. Membrane Transporter/Ion Channel
    Autophagy
  2. P-glycoprotein
    Autophagy
  3. Piperine

Piperine (Synonyms: Bioperine; 1-Piperoylpiperidine)

Cat. No.: HY-N0144 Purity: 98.94%
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

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Customer Review

Based on 8 publication(s) in Google Scholar

Top Publications Citing Use of Products

    Piperine purchased from MCE. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457. 

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

    Piperine purchased from MCE. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457. 

    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.

    Piperine purchased from MCE. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457. 

    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 MCE. Usage Cited in: Int Immunopharmacol. 2018 Oct 30;65:448-457. 

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

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    • 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].

    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 and t1/2of 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].

    Clinical Trial
    Molecular Weight

    285.34

    Formula

    C₁₇H₁₉NO₃

    CAS No.

    94-62-2

    SMILES

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

    Shipping

    Room temperature in continental US; may vary elsewhere.

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 31 mg/mL (108.64 mM)

    *"≥" means soluble, but saturation unknown.

    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
    10 mM 0.3505 mL 1.7523 mL 3.5046 mL
    *Please refer to the solubility information to select the appropriate solvent.
    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
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    Keywords:

    PiperineBioperine1-PiperoylpiperidineP-glycoproteinAutophagyP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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    Product name:
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