| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
Puerarin is a 5-HT2C receptor antagonist and also acts at the benzodiazepine site. It functions as a novel IK1 open channel blocker, which may underlie its antiarrhythmic actions. Additionally, it modulates inflammatory pathways by regulating NF-κB activation through I-κB phosphorylation. It has been shown to inhibit LPS-induced expression of iNOS, COX-2, and CRP in RAW264.7 cells. Puerarin also protects neurons against H₂O₂-induced oxidative stress and inhibits the activity of SH-SY5Y cells with an IC₅₀ of 174.4 μM.
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| ln Vitro |
Puerarin suppressed the mRNA of these cells in RT-PCR assays using RAW264.7, as well as the LPS-induced expression of iNOS, COX-2 cells, and CRP. I-κB phosphorylation and puerarin-mediated regulation of LPS-induced iNOS, COX-2, and CRP expression drift from the transcriptional level to regulate NF-κB activation are the causes of the inhibition of iNOS, COX-2, and CRP expression [1]. It is a novel kind of IK1 open channel blocker and could be the source of puerarin's antiarrhythmic action. IK1 current is dynamically inhibited by purerarin, an open channel inhibitor of IK1 [2].
In vitro, puerarin (25-200 µM) inhibits cell viability in a dose-dependent manner. It suppresses LPS-induced iNOS, COX-2, and CRP protein expression and mRNA levels in RAW264.7 cells via NF-κB pathway regulation. Puerarin (10-50 µM) protects H9c2 cells from hypoxia/reoxygenation injury by reducing LDH release. It also inhibits osteoclast formation in RAW264.7 cells induced by RANKL and stimulates osteogenesis in MC3T3-E1 preosteoblasts at concentrations of 10⁻⁹ to 10⁻⁷ M. |
| ln Vivo |
Due to their possible antioxidant, anti-inflammatory, or anti-cellular properties, genistein and puerarin both successfully reduce liver damage brought on by long-term alcohol-activated pathways. Genistein also decreased malondialdehyde (1.05±0.0947 vs. 1.28±0.213 nmol/mg pro, p<0.05), tumor cytokine α (3.12±0.498 vs. 3.82±0.277 pg/mg pro, p < 0.05), and interleukin-6 (1.46±0.223 vs. 1.88±0.309 pg/mg pro), p < 0.05). On the other hand, puerarin was superior to genistein in terms of raising serum activity or propionate aminotransferase levels (35.8±3.95 vs. 42.6) ±6.56 U/L, p < 0.05) and LDL carrot (1.12±0.160 vs. 1.55±0.150 mmol/L, p < 0.05)[3]. Puerarin has been shown to considerably ameliorate early renal damage [4], maybe through blocking the production of TNF-α and ICAM-1 in diabetic renin.
In vivo, oral administration of puerarin (300 mg/kg/day) to rats on a high-cholesterol diet significantly reduces the increase in total cholesterol levels in both serum and liver. Puerarin treatment (80 mg/kg/day) shows protective effects in various disease models. It ameliorates early renal damage, potentially by blocking TNF-α and ICAM-1 production. Puerarin (25 or 50 mg/kg) administered 10 min before MCAO provides neuroprotective effects. In ovariectomized mice, it prevents bone loss and increases social interaction time and locomotor activity in animal models of substance withdrawal. |
| Enzyme Assay |
Cell-free enzyme/receptor binding assays for puerarin typically involve radioligand binding displacement studies to determine affinity for the 5-HT2C receptor and other targets. Membranes prepared from cells expressing the receptor of interest are incubated with a radiolabeled ligand (e.g., [³H]-mesulergine for 5-HT2C) and varying concentrations of puerarin. Non-specific binding is determined in the presence of a saturating concentration of a reference compound. After incubation, the reaction is terminated by rapid filtration through glass fiber filters, and bound radioactivity is measured by scintillation counting to calculate IC₅₀ and Kᵢ values.
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| Cell Assay |
In vitro cellular assays for puerarin commonly use RAW264.7 macrophages to study anti-inflammatory effects. Cells are seeded in multi-well plates and pre-incubated with puerarin at various concentrations (e.g., 25-200 µM) for a designated period, followed by stimulation with LPS (e.g., 1 µg/mL). After incubation, the expression of iNOS, COX-2, and CRP is measured by Western blot or RT-PCR. Cell viability is assessed using CCK-8 or MTT assays. For neuroprotection studies, SH-SY5Y or H9c2 cells are treated with puerarin prior to exposure to H₂O₂ or hypoxia/reoxygenation injury.
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| Animal Protocol |
In vivo animal studies typically use rodent models. For the high-cholesterol diet model, rats are fed a high-cholesterol diet and concurrently administered puerarin (300 mg/kg/day) orally for a specified duration, after which serum and liver cholesterol levels are measured. For neuroprotection, rats undergo middle cerebral artery occlusion (MCAO) and receive puerarin (25 or 50 mg/kg) 10 min before the procedure. In the ovariectomized mouse model of bone loss, mice are ovariectomized and then treated with puerarin or 17β-estradiol for 4 weeks.
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| ADME/Pharmacokinetics |
Puerarin is an isoflavone C-glycoside with moderate oral bioavailability. It is typically formulated in 0.5% DMSO for in vitro studies and in a mixture of cremophor, ethanol, and normal saline (1:1:4) for in vivo administration. Its pharmacokinetic profile shows that it undergoes extensive metabolism, and its C-glycosidic bond contributes to its stability and longer half-life compared to O-glycosides. Puerarin is distributed to various tissues, including the brain, and is primarily excreted in urine and feces.
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| Toxicity/Toxicokinetics |
Puerarin has low acute toxicity and is generally well-tolerated in animal studies. In chronic administration, no significant adverse effects have been reported at therapeutic doses. The LD₅₀ in rodents is relatively high. Puerarin has been shown to protect against liver damage induced by long-term alcohol-activated pathways, suggesting hepatoprotective effects rather than hepatotoxicity. It also exhibits antioxidant properties that may mitigate oxidative stress-related damage. No significant genotoxicity or carcinogenicity has been reported.
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| References |
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| Additional Infomation |
Puerarin is a hydroxyisoflavone with the structure of isoflavone, where the 7' and 4' positions are substituted with hydroxyl groups, and the 8' position is linked by a β-D-glucopyranose residue via a C-glycosidic bond. It is a plant metabolite with autophagy-inducing, cardioprotective, antioxidant, anti-inflammatory, antipyretic, and ferroptosis-inhibiting effects. Puerarin is a C-glycoside compound and also a hydroxyisoflavone; its function is related to that of isoflavones, and it is the conjugate acid of puerarin(1-). Puerarin has been studied for the treatment of alcohol abuse. It has been reported to exist in Bupleurum chinense, Pueraria lobata, and other organisms with relevant data.
Puerarin (Standard) serves as a reference standard for analytical applications. The compound has been extensively studied for its therapeutic potential in cardiovascular diseases, diabetes, osteoporosis, neurodegenerative disorders, and cancer. It is a natural product found in Pueraria lobata and other organisms. The compound is a C-glycoside and a hydroxyisoflavone, and it is the conjugate acid of puerarin(1-). Despite extensive preclinical research, puerarin is not an FDA-approved drug but remains a compound of significant research interest. |
| Molecular Formula |
C21H20O9
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|---|---|
| Molecular Weight |
416.3781
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| Exact Mass |
416.1107
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| CAS # |
3681-99-0
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| PubChem CID |
5281807
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| Appearance |
White to off-white solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
791.2±60.0 °C at 760 mmHg
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| Melting Point |
187-189°C
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| Flash Point |
281.5±26.4 °C
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| Vapour Pressure |
0.0±2.9 mmHg at 25°C
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| Index of Refraction |
1.717
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| LogP |
-0.67
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
9
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
30
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| Complexity |
659
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1=CC(=CC=C1C2=COC3=C(C2=O)C=CC(=C3[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)O)O
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| Synonyms |
NPI 031G; NPI031G; NPI-031G
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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 : ~50 mg/mL (~120.08 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (7.20 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 30.0 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: ≥ 3 mg/mL (7.20 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. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 30.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. View More
Solubility in Formulation 3: 3 mg/mL (7.20 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. Solubility in Formulation 4: 20 mg/mL (48.03 mM) in 20% SBE-β-CD in Saline (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.4017 mL | 12.0083 mL | 24.0165 mL | |
| 5 mM | 0.4803 mL | 2.4017 mL | 4.8033 mL | |
| 10 mM | 0.2402 mL | 1.2008 mL | 2.4017 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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