| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
Luteolin 7-diglucuronide targets Protein Tyrosine Phosphatase 1B (PTP1B), a key regulator of insulin signaling and a therapeutic target for diabetes and metabolic disorders, with an IC₅₀ of 2.10 μM. The compound is approximately 13.5-fold more potent than luteolin aglycone. It also exhibits antioxidant, anti-inflammatory, cardioprotective, and neuroprotective activities. As a major flavonoid in verbena and lemon verbena, it contributes to the pharmacological properties of these plants.
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| ln Vitro |
Luteolin 7-diglucuronide demonstrates potent in vitro PTP1B inhibitory activity with an IC₅₀ of 2.10 μM, which is approximately 13.5-fold more potent than luteolin aglycone. This specific activity has not been reported for other major luteolin conjugates. The compound exhibits antioxidant, anti-inflammatory, cardioprotective, and neuroprotective effects. It has been shown to induce death in photoreceptor cells in certain contexts. The compound also has growth factor activity that stimulates tissue growth and wound healing.
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| ln Vivo |
In vivo studies have demonstrated that Luteolin 7-diglucuronide is orally bioavailable and effective in disease models. Oral administration at 40-150 mg/kg/day reduces fibrosis in mouse models. The compound's PTP1B inhibitory activity translates to in vivo efficacy for metabolic disorders and tissue fibrosis. Its antioxidant and anti-inflammatory properties contribute to protective effects in cardiovascular and neurological disease models. Further studies are needed to fully characterize its in vivo pharmacokinetic and pharmacodynamic profile across different disease indications.
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| Enzyme Assay |
In vitro enzyme/receptor binding (non-cell) assays for Luteolin 7-diglucuronide typically involve PTP1B inhibition studies. Recombinant human PTP1B protein is incubated with increasing concentrations of the compound (0.1-100 μM) and a synthetic substrate such as p-nitrophenyl phosphate (pNPP) in assay buffer (pH 7.0) at 37°C for 30-60 minutes. The reaction is stopped by the addition of NaOH, and the release of p-nitrophenol is measured spectrophotometrically at 405 nm. IC₅₀ values are determined from dose-response curves by nonlinear regression. Enzyme kinetics can be analyzed using Lineweaver-Burk plots to determine the mode of inhibition. Positive controls (e.g., known PTP1B inhibitors) and negative controls (buffer only) are included in each assay.
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| Cell Assay |
For in vitro cell-based assays, relevant cell lines (e.g., hepatocytes, adipocytes, or myocytes) are cultured in appropriate media. Cells are treated with Luteolin 7-diglucuronide at concentrations ranging from 1-100 μM for 24-48 hours. For insulin signaling studies, cells are stimulated with insulin with or without compound pretreatment. PTP1B activity in cell lysates is measured using phosphatase assay kits. Phosphorylation of insulin receptor and downstream signaling proteins (Akt, IRS-1) is analyzed by Western blot. Glucose uptake is assessed using 2-deoxyglucose uptake assays. Cell viability is measured by MTT or CCK-8 assays. Cytokine levels are measured by ELISA for anti-inflammatory studies.
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| Animal Protocol |
In vivo animal studies with Luteolin 7-diglucuronide typically use mouse models of fibrosis, metabolic disorders, or inflammation. The compound is administered orally at doses of 40-150 mg/kg/day for 2-4 weeks. For fibrosis studies, tissue fibrosis is induced by chemical agents (e.g., CCl₄) or surgical procedures. At study endpoint, tissues (liver, heart, kidney) are collected for histopathological analysis using Masson's trichrome or Sirius red staining to assess collagen deposition. Blood samples are collected for biochemical analysis of liver enzymes, glucose, and lipid profiles. Expression of fibrotic markers (TGF-β, collagen, α-SMA) is analyzed by qRT-PCR and Western blot. PTP1B activity in tissues is measured using phosphatase assays.
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| ADME/Pharmacokinetics |
Luteolin 7-diglucuronide is a flavonoid glycoside with a molecular weight of 638.5 g/mol and molecular formula C₂₇H₂₆O₁₈. The compound is orally bioavailable. As a glucuronide conjugate, it is more hydrophilic than luteolin aglycone, which may affect its absorption, distribution, metabolism, and excretion. The compound is the principal flavonoid constituent in Verbena officinalis and Aloysia triphylla. It is supplied as a phyproof® Reference Substance with ≥90.0% purity (HPLC) for analytical traceability. Storage at 2-8°C is recommended.
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| Toxicity/Toxicokinetics |
Luteolin 7-diglucuronide is considered to have a favorable safety profile as a naturally occurring flavonoid glycoside found in food and medicinal plants. At oral doses of 40-150 mg/kg/day in animal studies, the compound has been well-tolerated without significant adverse effects. As a component of commonly consumed herbs (verbena and lemon verbena), it has a history of safe use. No specific toxicity data are available for pure L7DG. The compound's antioxidant properties may provide protective effects against oxidative damage. High doses may cause gastrointestinal effects typical of flavonoid compounds.
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| References | |
| Additional Infomation |
Luteolin-7-O-[β-D-glucuronide-(1->2)-β-D-glucuronide] is a glycosyloxyflavonoid formed by the condensation of the 7-hydroxyl group of luteolin with the 1-position of 2-O-β-D-glucuronide-β-D-glucuronic acid. It is a trihydroxyflavonoid, glycosyloxyflavonoid, dicarboxylic acid, disaccharide derivative, and luteolin O-glucuronide. It is the conjugate acid of luteolin 7-O-[(β-D-glucuronic acid)-(1->2)-(β-D-glucuronic acid)]. Luteolin-7-O-[β-D-glucuronide-(1->2)-β-D-glucuronide] has been reported to be present in perilla, coleus, and other organisms with relevant data.
Luteolin 7-diglucuronide is a natural product standard suitable for Verbena and Aloysia analyses. Its identity is confirmed by the diglucuronide motif. The compound is a valuable tool for PTP1B pathway inhibition studies and serves as a metabolic probe for UGT1A1 pathway research. L7DG is the direct, validated tool compound for studying PTP1B in hepatic fibrosis or myocardial injury. It is supplied as an analytical reference standard and is not approved as a therapeutic drug. The compound is intended for research and analytical applications only. |
| Molecular Formula |
C27H26O18
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| Molecular Weight |
638.4845
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| Exact Mass |
638.111
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| CAS # |
96400-45-2
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| PubChem CID |
5282153
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| Appearance |
Yellow to brown solid powder
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| Density |
1.94±0.1 g/cm3
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| Boiling Point |
1101.6±65.0 °C
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| LogP |
-0.6
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
18
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
45
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| Complexity |
1150
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| Defined Atom Stereocenter Count |
10
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| SMILES |
C1=CC(=C(C=C1C2=CC(=O)C3=C(C=C(C=C3O2)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)C(=O)O)O)O)O[C@H]5[C@@H]([C@H]([C@@H]([C@H](O5)C(=O)O)O)O)O)O)O)O
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| InChi Key |
PBBVWJQPAZYQDB-DBFWEQBMSA-N
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| InChi Code |
InChI=1S/C27H26O18/c28-9-2-1-7(3-10(9)29)13-6-12(31)15-11(30)4-8(5-14(15)42-13)41-27-23(19(35)18(34)22(44-27)25(39)40)45-26-20(36)16(32)17(33)21(43-26)24(37)38/h1-6,16-23,26-30,32-36H,(H,37,38)(H,39,40)/t16-,17-,18-,19-,20+,21-,22-,23+,26-,27+/m0/s1
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| Chemical Name |
(2S,3S,4S,5R,6R)-6-[(2S,3R,4S,5S,6S)-6-carboxy-2-[2-(3,4-dihydroxyphenyl)-5-hydroxy-4-oxochromen-7-yl]oxy-4,5-dihydroxyoxan-3-yl]oxy-3,4,5-trihydroxyoxane-2-carboxylic acid
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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 Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ≥ 250 mg/mL (~391.55 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.5662 mL | 7.8311 mL | 15.6622 mL | |
| 5 mM | 0.3132 mL | 1.5662 mL | 3.1324 mL | |
| 10 mM | 0.1566 mL | 0.7831 mL | 1.5662 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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