| Size | Price | Stock | Qty |
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| Targets |
Natural biflavone; anti-inflammatory, anti-tumor, anti-oxidant, neuroprotective, anti-fungal activities
Ginkgetin targets multiple pathways and molecules. It has been identified as a potential inhibitor of the cGAS-STING pathway, which is involved in inflammation and senescence. It also inhibits arachidonate 5-lipoxygenase and cyclooxygenase 2. Furthermore, it is a potent inhibitor of Wnt signaling. Its anti-tumor effects are linked to the disruption of the Nrf2/HO-1 axis. |
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| ln Vitro |
Ginkgetin (2.5–20 μM; 48 hours) causes G2/M cell cycle arrest in Daoy cells and suppresses the growth of D283 and Daoy cell lines [2]. Osteosarcoma cells' apoptosis is markedly triggered by ginkgo (20–40 μM; 24 h) in a concentration-dependent manner [3]. In medulloblastoma cells, ginkgo (10–20 μM; 3–24 h) downregulates Wnt target gene expression without changing β-catenin expression [2]. In a concentration-dependent manner, ginkgo (1-10 μM) significantly inhibits the proliferation, migration, and wound recovery of endothelial cells induced by VEGF for 24 or 48 hours [1]. A549 cells die as a result of autophagy induced by ginkgo (5–10 μM; 48 hours) [5].
In vitro, Ginkgetin exhibits anti-tumor activity by enhancing the therapeutic effect of cisplatin in EGFR wild-type non-small-cell lung cancer via ferroptosis-mediated disruption of the Nrf2/HO-1 axis. It has also been shown to have senolytic action in human cell lines under various modalities of senescence. Its anti-inflammatory and neuroprotective activities have been demonstrated in various in vitro models. |
| ln Vivo |
Through the TLR4/NF-κB signaling pathway, ginkgo (25–100 mg/kg; intraperitoneally given two hours after ischemia) has anti-inflammatory effects on brain ischemia/reperfusion-induced damage in rat models [4]. ?In tumor-bearing nude mice, ginkgo (30 mg/kg; once daily gavage for 42 days) can prevent the formation of tumors in A549 cells [5].
In vivo, Ginkgetin has been shown to have anti-tumor, anti-inflammatory, and neuroprotective effects in animal models. However, specific in vivo experimental details, such as animal models and dosing regimens, are not provided in the search results. Its senolytic action has been validated in human cell lines, suggesting potential for in vivo efficacy. |
| Enzyme Assay |
In vitro enzyme/receptor binding assays for Ginkgetin have been used to identify its molecular targets. For example, a graph convolutional network-based drug "on-target" pathway prediction algorithm was employed to predict that the cGAS-STING pathway may be a potential target. Its inhibition of arachidonate 5-lipoxygenase and cyclooxygenase 2 has also been characterized.
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| Cell Assay |
Cell viability assay [2]
Cell Types: Daoy and D283 cell lines Tested Concentrations: 2.5, 5, 10, 20 μM Incubation Duration: 48 hrs (hours) Experimental Results: Inhibited cell growth, the IC50 of Daoy and D283 cells were 14.65 and 15.81 μM respectively. Apoptosis analysis [3] Cell Types: Osteosarcoma cells Tested Concentrations: 20, 30, 40 μM Incubation Duration: 24 hrs (hours) Experimental Results: Dramatically induced osteosarcoma cell apoptosis in a concentration-dependent manner. Cell cycle analysis [2] Cell Types: Daoy cells Tested Concentrations: 2.5, 5, 10, 20 μM Incubation Duration: 24 hrs (hours) Experimental Results: Compared with the control, the G2/M phase increased, indicating G2/M cell phase arrest. Cell cycle analysis [2] Cell Types: Daoy and D283 cell lines Tested Concentrations: 10, 20 μM Incubation Duration: 3, 6, 12, 24 hrs (hours) Experimental Results: The expression of Wnt target genes, Axin2, cyclin D1 and survivin was attenuated at 20 μM. Daoy cells for 24 hrs (hours). Does not affect total beta-catenin levels and reduces beta-catenin phosphorylation levels in a time- and concentration-depen In vitro cell-based assays for Ginkgetin involve treating various human cell lines with the compound to assess its effects on cell viability, senescence, and other cellular processes. Cytotoxicity assays and western blotting are used to study its mechanism of action, such as its role in ferroptosis and the Nrf2/HO-1 axis. |
| Animal Protocol |
Animal/Disease Models: Male SD (SD (Sprague-Dawley)) rat (200-220 g) [4]
Doses: 25, 50, 100 mg/kg Route of Administration: intraperitoneal (ip) injection 2 hrs (hrs (hours)) after ischemia. Experimental Results: diminished neurological deficit score. Inhibits the expression of NF-κB, TLR4 and IκBα in the ischemic penumbra cortex, and inhibits the degradation of IκBα. Reduce the expression of ICAM-1, COX-2 and iNOS. Downregulates the expression of downstream inflammatory factors PGE2 and TNF-α. IL-1β, IL-6, IL-8, and IL-10 protein expression was diminished. In vivo animal experiments for Ginkgetin have been conducted in models of disease, though specific details are not provided in the search results. The compound is typically administered orally or via injection, and its effects on disease progression and related biomarkers are assessed. |
| ADME/Pharmacokinetics |
Ginkgetin is soluble in DMSO (50 mg/mL). Its pharmacokinetic properties, including absorption, distribution, metabolism, and excretion, have not been detailed in the available search results. As a natural product, its bioavailability and metabolic stability may vary depending on the route of administration.
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| Toxicity/Toxicokinetics |
No specific toxicity data is provided for Ginkgetin in the search results. As a natural compound, it may have a relatively favorable safety profile, but detailed toxicological studies would be required for clinical development. It has been used in research settings for its various biological activities.
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| References |
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| Additional Infomation |
Ginkgo flavonoids are biflavonoid compounds, specifically a 7,4'-dimethyl ether derivative of ferulic acid flavonoids. Isolated from ginkgo leaves and dihydroquercetin, they possess anti-HSV-1, antitumor, and inhibitory activities against arachidonic acid 5-lipoxygenase and cyclooxygenase 2. They can function as an anti-HSV-1 drug, a cyclooxygenase 2 inhibitor, an EC 1.13.11.34 (arachidonic acid 5-lipoxygenase) inhibitor, an antitumor drug, and a metabolite. It is a biflavonoid compound, and also a hydroxyflavonoid, methoxyflavonoid, and cyclic compound. Its functions are related to ferulic acid flavonoids. Ginkgo flavonoids have been reported to exist in Selaginella, Taxus, and other organisms with relevant data.
Ginkgetin is a bioactive biflavone from Ginkgo biloba with diverse pharmacological properties, including anti-tumor, anti-inflammatory, and neuroprotective activities. It is a potent inhibitor of Wnt signaling and has been identified as a potential senolytic agent. It is a research compound and has not been approved for clinical use. |
| Molecular Formula |
C32H22O10
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|---|---|
| Molecular Weight |
566.518
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| Exact Mass |
566.121
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| Elemental Analysis |
C, 67.84; H, 3.91; O, 28.24
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| CAS # |
481-46-9
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| PubChem CID |
5271805
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.5±0.1 g/cm3
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| Boiling Point |
863.7±65.0 °C at 760 mmHg
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| Melting Point |
336ºC
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| Flash Point |
287.2±27.8 °C
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| Vapour Pressure |
0.0±0.3 mmHg at 25°C
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| Index of Refraction |
1.714
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| LogP |
4.45
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
10
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
42
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| Complexity |
1080
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
AIFCFBUSLAEIBR-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C32H22O10/c1-39-18-10-20(34)30-23(37)13-27(41-28(30)11-18)16-5-8-25(40-2)19(9-16)29-21(35)12-22(36)31-24(38)14-26(42-32(29)31)15-3-6-17(33)7-4-15/h3-14,33-36H,1-2H3
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| Chemical Name |
5,7-dihydroxy-8-[5-(5-hydroxy-7-methoxy-4-oxochromen-2-yl)-2-methoxyphenyl]-2-(4-hydroxyphenyl)chromen-4-one
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| Synonyms |
Ginkgetin; 481-46-9; 7,4'-Dimethylamentoflavone; Amentoflavone 7,4'-dimethyl ether; CHEBI:5353; HY5EZW8269; 5,7-dihydroxy-8-[5-(5-hydroxy-7-methoxy-4-oxochromen-2-yl)-2-methoxyphenyl]-2-(4-hydroxyphenyl)chromen-4-one; 4H-1-Benzopyran-4-one, 5,7-dihydroxy-8-(5-(5-hydroxy-7-methoxy-4-oxo-4H-1-benzopyran-2-yl)-2-methoxyphenyl)-2-(4-hydroxyphenyl)-;
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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 : ≥ 20.83 mg/mL (~36.77 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2 mg/mL (3.53 mM) in 50% PEG300 + 50% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with heating and sonication.
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 mg/mL (3.53 mM) in 0.5% CMC-Na/saline water (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication (<60°C). Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O 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 | 1.7652 mL | 8.8258 mL | 17.6516 mL | |
| 5 mM | 0.3530 mL | 1.7652 mL | 3.5303 mL | |
| 10 mM | 0.1765 mL | 0.8826 mL | 1.7652 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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