| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| Other Sizes |
| Targets |
Oroxylin 7-O-glucoside exhibits its biological effects through multiple signaling pathways. The compound inhibits the JNK pathway, upregulates PPARγ, and inhibits NF-κB p65 nuclear translocation. It reduces the production of pro-inflammatory cytokines including IL-1β and IL-6. As a flavonoid glucuronide, it interacts with various enzymes and receptors through its antioxidant properties, involving scavenging of free radicals and modulation of redox-sensitive signaling pathways. The compound also exhibits prolyl oligopeptidase (POP) inhibitory activity.
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|---|---|
| ln Vitro |
In vitro studies have demonstrated that Oroxylin 7-O-glucoside possesses broad-spectrum antiviral activity against hepatitis B virus (HBV), herpes simplex virus type 2 (HSV-2), and influenza H3N2. In direct comparative studies, it demonstrated significantly greater antiviral potency than baicalin against both HBV and HSV-2. The compound also exhibits anti-inflammatory, anticancer, neuroprotective, and hepatoprotective activities. Its anti-angiogenic and antitumor effects have been investigated in glioma and hepatocellular carcinoma models.
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| ln Vivo |
In vivo studies have shown that Oroxylin 7-O-glucoside achieves superior oral pharmacokinetics, attaining the highest systemic exposure despite low oral doses. The compound's singular microbial deglycosylation pathway yields cleaner metabolic data compared to the multi-pathway complexity of baicalin. It has been studied for its hepatoprotective effects in animal models of liver injury. The favorable oral pharmacokinetic profile makes it a compound of high interest for in vivo virology and pharmacokinetics research.
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| Enzyme Assay |
In vitro receptor binding studies for Oroxylin 7-O-glucoside typically employ radioligand binding assays or surface plasmon resonance to evaluate interactions with target proteins such as PPARγ and NF-κB pathway components. Enzyme inhibition assays are performed using purified prolyl oligopeptidase (POP) with fluorogenic substrates to determine IC₅₀ values. Binding affinity to α-hemolysin is assessed using hemolytic activity inhibition assays. Competitive binding experiments with specific inhibitors are used to confirm target specificity and characterize binding kinetics.
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| Cell Assay |
Cellular assays for Oroxylin 7-O-glucoside are performed using relevant cell lines including hepatocytes (for HBV studies), Vero cells (for HSV-2 studies), and cancer cell lines (for antitumor studies). Cells are cultured in appropriate media and treated with compound concentrations ranging from 1-200 μM. Antiviral activity is assessed by measuring viral load using qPCR or plaque reduction assays. Anti-inflammatory activity is evaluated by measuring cytokine levels (IL-1β, IL-6) in culture supernatants using ELISA. Cell viability and proliferation are assessed using MTT or CCK-8 assays.
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| Animal Protocol |
In vivo animal studies for Oroxylin 7-O-glucoside have been conducted in mouse and rat models. The compound is typically administered orally at doses determined from pharmacokinetic studies. For antiviral efficacy studies, animals are infected with HBV, HSV-2, or influenza virus and treated with the compound for 7-14 days. Viral load is measured in serum or tissue samples using qPCR. For hepatoprotective studies, liver injury is induced using CCl₄ or other hepatotoxins, and liver function markers (ALT, AST) are measured. Tissue samples are collected for histopathological analysis.
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| ADME/Pharmacokinetics |
Pharmacokinetic studies of Oroxylin 7-O-glucoside have demonstrated superior oral bioavailability compared to related flavonoids such as baicalin and wogonoside. The compound achieves the highest systemic exposure despite low oral doses, indicating efficient absorption. Its unique microbial deglycosylation pathway, where the glucuronide moiety is cleaved by gut microbiota prior to absorption of the aglycone, yields more predictable metabolic profiles. The compound is metabolized to Oroxylin A, which is further subject to phase II conjugation.
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| Toxicity/Toxicokinetics |
Specific toxicity data for Oroxylin 7-O-glucoside are limited in the published literature. As a naturally occurring flavonoid from Scutellaria baicalensis, a widely used medicinal herb with a long history of safe use, the compound is expected to have a favorable safety profile. Standard toxicological assessments would include acute toxicity studies in rodents, repeated-dose toxicity studies, genotoxicity testing (Ames test, micronucleus assay), and hERG channel binding assessment for cardiac safety. The compound is intended for research use only and is not approved for human therapeutic applications.
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| References | |
| Additional Infomation |
Oroxylin 7-O-glucoside is distinguished by its broad-spectrum antiviral activity against HBV, HSV-2, and H3N2, with potency superior to baicalin. Its mechanism of action involves JNK pathway inhibition, PPARγ upregulation, and NF-κB p65 nuclear translocation inhibition. The compound's favorable oral pharmacokinetics, characterized by high systemic exposure despite low doses, make it a promising lead for antiviral drug development. It also exhibits anti-angiogenic, antitumor, anti-inflammatory, and hepatoprotective effects. The compound is not currently approved for clinical use; all applications remain at the preclinical research stage.
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| Molecular Formula |
C22H22O10
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|---|---|
| Molecular Weight |
446.404
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| Exact Mass |
446.121
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| CAS # |
36948-77-3
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| PubChem CID |
101101153
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| Appearance |
green yellow solid
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| Source |
Originated from plants: Compositae Carlina acaulis L.
Originated from plants: Labiatae |
| LogP |
1.2
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
|
| Heavy Atom Count |
32
|
| Complexity |
692
|
| Defined Atom Stereocenter Count |
5
|
| SMILES |
COC1=C(C=C2C(=C1O)C(=O)C=C(O2)C3=CC=CC=C3)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O
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| InChi Key |
RQZJKRNQAPBBAP-IWLDQSELSA-N
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| InChi Code |
InChI=1S/C22H22O10/c1-29-21-14(31-22-20(28)19(27)17(25)15(9-23)32-22)8-13-16(18(21)26)11(24)7-12(30-13)10-5-3-2-4-6-10/h2-8,15,17,19-20,22-23,25-28H,9H2,1H3/t15-,17-,19+,20-,22-/m1/s1
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| Chemical Name |
5-hydroxy-6-methoxy-2-phenyl-7-[(2S,3R,4S,5S,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]oxychromen-4-one
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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: ~15 mg/mL (~33.6 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.60 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (25.0 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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 (5.60 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 DMSO stock solution (25.0 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2401 mL | 11.2007 mL | 22.4014 mL | |
| 5 mM | 0.4480 mL | 2.2401 mL | 4.4803 mL | |
| 10 mM | 0.2240 mL | 1.1201 mL | 2.2401 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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