| Size | Price | Stock | Qty |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg |
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| 1g |
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| Other Sizes |
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Purity: ≥98%
Piperlongumine (Piplartine) is an naturally occurring and biologically active alkaloid that has been isolated from peppers, particularly long peppers like Piper longum Linn. It has anti-inflammatory, antibacterial, antiangiogenic, antioxidant, antitumor, and anti-diabetic properties. In cancer cell lines, piperlongumine causes the production of ROS and apoptosis. Piperlongumine inhibits myofibroblast transformation by blocking the ERK1/2 signaling pathway and exhibits anti-cardiac fibrosis activity. Ayurvedic medicine, which is used to treat a variety of illnesses, including tumors, uses long pepper as one of its most popular herbs. The pharmacological effects of piplartine have been described as including cytotoxic, genotoxic, antitumor, antiangiogenic, antimetastatic, antiplatelet aggregation, antinociceptive, anxiolytic, antidepressant, anti-atherosclerotic, antidiabetic, antibacterial, antifungal, leishmanicidal, trypanocidal, and schistosomicidal effects. The most promising of piplartine's numerous pharmacological effects is its ability to fight cancer.
| Targets |
reactive oxygen species (ROS); TrxR1; CRM1; PI3K/Akt/mTOR
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|---|---|
| ln Vitro |
Piperlongumine is a known ROS inducer that has the potential to cause the death of pancreatic cancer cells in culture[1] Platelet aggregation is prevented by piperlongumine, a thromboxane A(2) receptor antagonist. [2] In addition to promoting autophagy and mediating cancer cell death, piperlongumine inhibits Akt/mTOR signalling.[3]
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| ln Vivo |
Piperlongumine (50 mg/kg i.p.) causes tumor cell in vivo growth inhibition without significantly altering biochemical, hematological, or histopathological parameters. [4]
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| Cell Assay |
Various PL concentrations are incubated with MCF-7 and 786-O cells for 48 hours. CellTiter Blue assay is used to analyze cell proliferation. With the help of the Microsoft Excel add-in XLift, effective doses (ED) are calculated.
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| Animal Protocol |
Mice transplanted with sarcoma 180 tumors
~50 mg/kg i.p. |
| References |
| Molecular Formula |
C17H19NO5
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|---|---|
| Molecular Weight |
317.3365
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| Exact Mass |
317.13
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| Elemental Analysis |
C, 64.34; H, 6.03; N, 4.41; O, 25.21
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| CAS # |
20069-09-4
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| Related CAS # |
20069-09-4
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| Appearance |
Solid powder
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| SMILES |
COC1=CC(=CC(=C1OC)OC)/C=C/C(=O)N2CCC=CC2=O
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| InChi Key |
VABYUUZNAVQNPG-BQYQJAHWSA-N
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| InChi Code |
InChI=1S/C17H19NO5/c1-21-13-10-12(11-14(22-2)17(13)23-3)7-8-16(20)18-9-5-4-6-15(18)19/h4,6-8,10-11H,5,9H2,1-3H3/b8-7+
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| Chemical Name |
1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one
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| Synonyms |
Piperlongumine; Piplartine
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 63~100 mg/mL (198.5~315.1 mM)
Ethanol: ~63 mg/mL (~198.5 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.88 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (7.88 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (6.55 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 2% DMSO+40% PEG 300+2% Tween 80+ddH2O: 5mg/mL |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1512 mL | 15.7560 mL | 31.5119 mL | |
| 5 mM | 0.6302 mL | 3.1512 mL | 6.3024 mL | |
| 10 mM | 0.3151 mL | 1.5756 mL | 3.1512 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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