Piperine (Synonyms: Bioperine; 1-Piperoylpiperidine)

Name: Piperine
Brand: MedChemExpress
SKU: HY-N0144
Rating: 5.0 (15 reviews)

Cat. No.: HY-N0144 Purity: 98.88%: FAQs
Data Sheet SDS COA Handling Instructions

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Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC₅₀ of 61.94±0.054 μg/mL.

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

Piperine Chemical Structure

CAS No. : 94-62-2

Size	Price	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	USD 33	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	USD 33	In-stock	Estimated Time of Arrival: December 31
Solid
5 g	USD 30	In-stock	Estimated Time of Arrival: December 31
10 g	USD 50	In-stock	Estimated Time of Arrival: December 31
50 g		Get quote

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Based on 15 publication(s) in Google Scholar

Other Forms of Piperine:

Isochavicine Get quote
(E/Z)-Piperine Get quote
Piperin-d₁₀ Get quote
Piperine (Standard) Get quote

11 Publications Citing Use of MCE Piperine

: 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 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 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 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.

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Description

Piperine is an alkaloid, can be isolated from pepper. Piperine can inhibit the activity of P-glycoprotein and CYP3A4. Piperine inhibits HeLa cells with an IC₅₀ of 61.94±0.054 μg/mL^[1]^[2]^[3].

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	11.89 μM Compound: Piperine	Antiproliferative activity in human A549 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay Antiproliferative activity in human A549 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay	[PMID: 30108756]
Bel-7402	IC₅₀	> 10 μM Compound: Piperine	Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human Bel-7402 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33026807]
BTI-TN-5B1-4	IC₅₀	1.05 μM Compound: 1	Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho Inhibition of human microsomal MAO-B expressed in baculovirus infected BTI-TN-5B1-4 cells assessed as reduction in 4-hydroxyquinoline formation using kynuramine as substrate preincubated with substrate for 10 mins followed by enzyme addition by spectropho	[PMID: 31711793]
COLO 205	IC₅₀	46 μM Compound: 1	Cytotoxicity against Homo sapiens (human) COLO205 cells by SRB assay Cytotoxicity against Homo sapiens (human) COLO205 cells by SRB assay	10.1007/s00044-010-9500-5
DLD-1	IC₅₀	< 200 μM Compound: 58	Anticancer activity against human DLD-1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Anticancer activity against human DLD-1 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 33445154]
DU-145	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against Homo sapiens (human) DU145 cells by SRB assay Cytotoxicity against Homo sapiens (human) DU145 cells by SRB assay	10.1007/s00044-010-9500-5
HCT-116	IC₅₀	< 200 μM Compound: 58	Anticancer activity against human HCT-116 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Anticancer activity against human HCT-116 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 33445154]
HeLa	IC₅₀	0.95 μM Compound: 1	Cytotoxicity against Homo sapiens (human) HeLa cells after 48 hr by MTT assay Cytotoxicity against Homo sapiens (human) HeLa cells after 48 hr by MTT assay	10.1007/s00044-013-0541-4
HeLa	IC₅₀	19.21 μM Compound: Piperine	Antiproliferative activity in human HeLa cells assessed as reduction in cell number incubated for 48 hrs by SRB assay Antiproliferative activity in human HeLa cells assessed as reduction in cell number incubated for 48 hrs by SRB assay	[PMID: 30108756]
HEp-2	IC₅₀	70 μM Compound: 1	Cytotoxicity against Homo sapiens (human) Hep2 cells by SRB assay Cytotoxicity against Homo sapiens (human) Hep2 cells by SRB assay	10.1007/s00044-010-9500-5
Hepatocyte	IC₅₀	12 μM Compound: 10	Hepatoprotective activity in ddY mouse hepatocytes assessed as inhibition of D-galactosamine/TNFalpha-induced cytotoxicity after 20 hrs by MTT assay relative to untreated control Hepatoprotective activity in ddY mouse hepatocytes assessed as inhibition of D-galactosamine/TNFalpha-induced cytotoxicity after 20 hrs by MTT assay relative to untreated control	[PMID: 19775895]
HepG2	IC₅₀	> 10 μM Compound: Piperine	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 33026807]
HUVEC	IC₅₀	100 μM Compound: Piperine	Antiinflammatory activity in HUVEC assessed as inhibition of TNFalpha-induced ICAM-1 expression incubated for 2 hrs prior to TNFalpha challenge measured after 16 hrs by ELISA Antiinflammatory activity in HUVEC assessed as inhibition of TNFalpha-induced ICAM-1 expression incubated for 2 hrs prior to TNFalpha challenge measured after 16 hrs by ELISA	10.1039/C2MD20216F
IMR-32	IC₅₀	10.19 μM Compound: Piperine	Antiproliferative activity in human IMR32 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay Antiproliferative activity in human IMR32 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay	[PMID: 30108756]
IMR-32	IC₅₀	89 μM Compound: 1	Cytotoxicity against Homo sapiens (human) IMR32 cells by SRB assay Cytotoxicity against Homo sapiens (human) IMR32 cells by SRB assay	10.1007/s00044-010-9500-5
L929	IC₅₀	42 μM Compound: 10	Cytoprotective activity in mouse L929 cells assessed as inhibition of TNF-alpha-induced cytotoxicity by MTT assay relative to untreated control Cytoprotective activity in mouse L929 cells assessed as inhibition of TNF-alpha-induced cytotoxicity by MTT assay relative to untreated control	[PMID: 19775895]
MCF7	IC₅₀	0.99 μM Compound: 1	Cytotoxicity against Homo sapiens (human) MCF7 cells after 48 hr by MTT assay Cytotoxicity against Homo sapiens (human) MCF7 cells after 48 hr by MTT assay	10.1007/s00044-013-0541-4
MCF7	IC₅₀	12.96 μM Compound: Piperine	Antiproliferative activity in human MCF7 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay Antiproliferative activity in human MCF7 cells assessed as reduction in cell number incubated for 48 hrs by SRB assay	[PMID: 30108756]
MCF7	IC₅₀	99 μM Compound: 1	Cytotoxicity against Homo sapiens (human) MCF7 cells by SRB assay Cytotoxicity against Homo sapiens (human) MCF7 cells by SRB assay	10.1007/s00044-010-9500-5
MDA-MB-231	IC₅₀	58.45 μg/mL Compound: 3	Cytotoxicity against Homo sapiens (human) MDA-MB-231 cells assessed as growth inhibition by MTT assay Cytotoxicity against Homo sapiens (human) MDA-MB-231 cells assessed as growth inhibition by MTT assay	10.1007/s00044-012-0397-z
Oocyte	EC₅₀	52 μM Compound: 5	Activation of rat GABA alpha-1-beta-2-gamma-2 receptor expressed in xenopus oocytes assessed as potentiation of GABA-induced chloride current after 90 secs by two microplate electrode voltage clamp assay Activation of rat GABA alpha-1-beta-2-gamma-2 receptor expressed in xenopus oocytes assessed as potentiation of GABA-induced chloride current after 90 secs by two microplate electrode voltage clamp assay	[PMID: 20085307]
PC-3	IC₅₀	> 50 μM Compound: 1	Cytotoxicity against Homo sapiens (human) PC3 cells by SRB assay Cytotoxicity against Homo sapiens (human) PC3 cells by SRB assay	10.1007/s00044-010-9500-5
SW480	IC₅₀	< 200 μM Compound: 58	Anticancer activity against human SW480 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Anticancer activity against human SW480 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 33445154]

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 AUC_0→t is unproportionally increased with doses, indicating a potential non-linear pharmacokinetics profile of piperine. It is found that the AUC_0→t and C₀ of Docetaxel (HY-B0011) and t_1/2 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.

94-62-2

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

Endogenous metabolite

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
10 mM	0.3505 mL	1.7523 mL	3.5046 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)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (8.76 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

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mg/kg

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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%

Select Batch:

Data Sheet (278 KB) SDS (393 KB)

COA (245 KB) LCMS (278 KB)

Handling Instructions (2659 KB)

References

[1]. Paarakh PM, et al. In vitro cytotoxic and in silico activity of piperine isolated from Piper nigrum fruits Linn. In Silico Pharmacol. 2015 Dec;3(1):9. Epub 2015 Oct 29. [Content Brief]

[2]. Meghwal M,et al. Piper nigrum and piperine: an update. Phytother Res. 2013 Aug;27(8):1121-30. [Content Brief]

[3]. Li C, et al. Non-linear pharmacokinetics of piperine and its herb-drug interactions with docetaxel in Sprague-Dawley rats. J Pharm Biomed Anal. 2016 Sep 5;128:286-93. [Content Brief]

[4]. Zhai WJ, et al. Piperine Plays an Anti-Inflammatory Role in Staphylococcus aureus Endometritis by Inhibiting Activation of NF-κB and MAPK Pathways in Mice. Evid Based Complement Alternat Med. 2016;2016:8597208. [Content Brief]

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	[1]. Paarakh PM, et al. In vitro cytotoxic and in silico activity of piperine isolated from Piper nigrum fruits Linn. In Silico Pharmacol. 2015 Dec;3(1):9. Epub 2015 Oct 29. [Content Brief] [2]. Meghwal M,et al. Piper nigrum and piperine: an update. Phytother Res. 2013 Aug;27(8):1121-30. [Content Brief] [3]. Li C, et al. Non-linear pharmacokinetics of piperine and its herb-drug interactions with docetaxel in Sprague-Dawley rats. J Pharm Biomed Anal. 2016 Sep 5;128:286-93. [Content Brief] [4]. Zhai WJ, et al. Piperine Plays an Anti-Inflammatory Role in Staphylococcus aureus Endometritis by Inhibiting Activation of NF-κB and MAPK Pathways in Mice. Evid Based Complement Alternat Med. 2016;2016:8597208. [Content Brief]

Complete Stock Solution Preparation Table

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

Piperine 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:

Piperine94-62-2Bioperine 1-PiperoylpiperidineP-glycoproteinAutophagyEndogenous MetaboliteP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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Piperine (Synonyms: Bioperine; 1-Piperoylpiperidine)

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Other Forms of Piperine:

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11 Publications Citing Use of MCE Piperine

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