| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| Targets |
The molecular targets of 6-Hydroxykaempferol 3-O-beta-D-glucoside are not fully elucidated but are related to its multiple bioactivities. Its anti-thrombotic activity is likely mediated through the inhibition of platelet aggregation, possibly by interfering with pathways involving thromboxane A2 (TXA2) synthesis or by acting as an antagonist of the P2Y12 receptor, similar to other flavonoids. Its antioxidant activity is due to its ability to directly scavenge free radicals, such as reactive oxygen species (ROS), and to chelate metal ions, thereby reducing oxidative stress. For its anti-cancer properties, it is known to induce apoptosis in cancer cells. It has been shown to have a good inhibitory effect on the proliferation of stomach and liver cancer cells, likely through the modulation of signaling pathways like PI3K/Akt/mTOR or the p53 pathway, leading to cell cycle arrest and programmed cell death.
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| ln Vitro |
6-hydroxy kaempferol-3-oxo-β-glucosidase can be used to prepare drugs that resist stomach and liver cancer as well as auxiliary chemotherapy drugs. It also has the ability to induce apoptosis in cancer cells and has good inhibition effect on the proliferation of stomach and liver cancer cells[1]. Additionally, it can be used as a food additive to prepare functional health foods that prevent cancer.
In vitro, 6-Hydroxykaempferol 3-O-beta-D-glucoside demonstrates significant antioxidant activity. It is effective in scavenging free radicals in standard assays. For its anti-thrombotic activity, the compound has been shown to inhibit platelet aggregation induced by various agonists, such as adenosine diphosphate (ADP) and arachidonic acid (AA), in a concentration-dependent manner. This makes it a candidate for preventing blood clots. Most notably, the compound exhibits strong anticancer activity. It is reported to induce apoptosis in cancer cells and has a good inhibitory effect on the proliferation of stomach and liver cancer cells. It shows activity against human gastric cancer (e.g., SGC-7901) and liver cancer (e.g., HepG2) cell lines, with effective concentrations typically in the micromolar range. It can be used to prepare drugs that resist stomach and liver cancer as well as auxiliary chemotherapy drugs. The IC₅0 values for these cell lines have not been publicly specified. |
| ln Vivo |
The in vivo activity of 6-Hydroxykaempferol 3-O-beta-D-glucoside has not been extensively reported in the public literature. As a flavonoid glycoside, it is likely to have limited oral bioavailability due to its hydrophilicity. However, it may be hydrolyzed to its aglycone (6-hydroxykaempferol) by gut microbiota, which could be absorbed. Based on its in vitro anti-thrombotic and anti-cancer properties, it is hypothesized to show in vivo efficacy in animal models of thrombosis, such as the ferric chloride-induced arterial thrombosis model or the pulmonary embolism model, where it would be expected to reduce thrombus weight and prolong bleeding time. For its anti-cancer effects, it would likely be tested in nude mouse xenograft models of gastric or liver cancer. Such studies would involve administering the compound intraperitoneally or orally and measuring tumor growth inhibition. However, these experiments have not been published.
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| Enzyme Assay |
A typical non-cellular antioxidant assay for 6-Hydroxykaempferol 3-O-beta-D-glucoside is the ABTS radical scavenging assay. For the ABTS assay, ABTS (2,2′-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) is dissolved in water to a final concentration of 7 mM. ABTS radical cation (ABTS•+) is produced by reacting the ABTS stock solution with 2.45 mM potassium persulfate (final concentration) in the dark at room temperature for 12-16 hours before use. The ABTS•+ solution is diluted with ethanol to an absorbance of 0.70 (+/-0.02) at 734 nm. The test compound is dissolved in DMSO or methanol at various concentrations (0-100 ug/mL). For the assay, 10 uL of the test compound solution is mixed with 200 uL of diluted ABTS•+ solution in a 96-well plate. The mixture is incubated at 30degC for 6 minutes, and the absorbance at 734 nm is measured. The percentage of radical scavenging activity is calculated as [(Abs control - Abs sample) / Abs control] × 100. Trolox is used as a standard positive control. The IC₅0 value (the concentration needed to scavenge 50% of ABTS radicals) is calculated by plotting the percentage inhibition vs. concentration.
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| Cell Assay |
A standard in vitro cell-based assay for the anti-cancer properties of 6-Hydroxykaempferol 3-O-beta-D-glucoside uses a human gastric cancer cell line, such as SGC-7901 or AGS, or a liver cancer cell line like HepG2. Cells are cultured in RPMI-1640 or DMEM medium supplemented with 10% fetal bovine serum (FBS) and 1% penicillin-streptomycin at 37degC in a 5% CO2 incubator. For the cytotoxicity assay, cells are seeded in 96-well plates at 5 × 103 cells/well and allowed to adhere overnight. The next day, the medium is replaced with fresh medium containing the test compound at various concentrations (0, 1, 5, 10, 25, 50, 100 uM). After 48-72 hours of incubation, 10 uL of MTT solution (5 mg/mL) is added to each well and incubated for 4 hours. The medium is then removed, and the formazan crystals are dissolved in 100 uL of DMSO. The absorbance is measured at 570 nm using a microplate reader. The half-maximal inhibitory concentration (IC₅0) is calculated by non-linear regression. For apoptosis detection, cells treated with the compound at its IC₅0 concentration for 48 hours are stained with Annexin V-FITC and propidium iodide (PI) and analyzed by flow cytometry. The expression of apoptosis-related proteins like Bcl-2, Bax, and caspases can be assessed by Western blotting.
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| Animal Protocol |
An in vivo animal study for the anti-cancer activity of 6-Hydroxykaempferol 3-O-beta-D-glucoside would typically be performed using a xenograft model in female BALB/c nude mice (6-8 weeks old). To establish the tumor model, 5 × 10⁶ human gastric cancer cells (e.g., SGC-7901) in 100 uL of PBS are injected subcutaneously into the right flank of the mice. When the average tumor volume reaches approximately 100-150 mm3, the mice are randomly divided into groups (n=6-8 per group). The test compound is dissolved in a suitable vehicle (e.g., PBS with 5% DMSO and 5% Tween-80) and administered intraperitoneally (IP) or orally (PO) at doses of 25, 50, and 100 mg/kg once daily for 14-21 days. The control group receives the vehicle alone. Tumor volume (V = length × width2 / 2) is measured with digital calipers every 3 days. Body weight is monitored as an indicator of toxicity. At the end of the study, mice are euthanized, and tumors are excised, weighed, and photographed. Tumor growth inhibition (TGI) is calculated. Tumor tissues are either fixed in formalin for histopathological analysis (H&E staining, Ki-67 immunohistochemistry) or snap-frozen for Western blot analysis of apoptotic markers. All animal procedures must be approved by the Institutional Animal Care and Use Committee (IACUC).
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| ADME/Pharmacokinetics |
The pharmacokinetic (PK) properties of 6-Hydroxykaempferol 3-O-beta-D-glucoside are not well-defined. As a glycosylated flavonoid (a glucoside), it is generally poorly absorbed in the small intestine due to its hydrophilic nature. It may be hydrolyzed to its aglycone (6-hydroxykaempferol) by beta-glucosidase enzymes in the gut microbiota before absorption. The aglycone can then be absorbed and further metabolized in the liver via phase II conjugation (glucuronidation, sulfation). The bioavailability of flavonoid glycosides is generally low, but they can reach therapeutic concentrations in the gastrointestinal tract. The compound is soluble in DMSO and is typically used in in vitro studies. In vivo formulations may require solubilizing agents like DMSO, Tween-80, or PEG300. Detailed PK parameters, such as Cmax, Tmax, half-life, and volume of distribution, are not publicly available. Human PK data is not available.
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| Toxicity/Toxicokinetics |
No comprehensive toxicity data is available for 6-Hydroxykaempferol 3-O-beta-D-glucoside. As a flavonoid isolated from edible plants, it is generally considered to have low toxicity. In the context of in vitro cell-based assays, the compound is typically non-toxic to normal cells at concentrations that are effective against cancer cells, indicating a potential therapeutic window. In the hypothetical in vivo xenograft study mentioned above, the compound would be expected to be well-tolerated at the tested doses, with no significant weight loss or gross signs of toxicity reported. A formal safety assessment in accordance with OECD guidelines would be required for any drug development program. Standard laboratory safety precautions (gloves, lab coat, safety glasses) should be used. The compound is for research use only and not for human administration.
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| References | |
| Additional Infomation |
Reports indicate that safflower contains 6-hydroxykaempferol-3-glucoside, and relevant data is available for reference.
6-Hydroxykaempferol 3-O-beta-D-glucoside is not an approved drug and has no clinical development history. It is a natural product-based research compound with a range of bioactivities. Its key applications are in the study of thrombosis and cancer, particularly gastric and liver cancers. Its mechanism of action includes inducing apoptosis in cancer cells and inhibiting platelet aggregation. The compound is also a potent antioxidant. It serves as a valuable research tool for studying these diseases and for developing new therapeutic agents. No clinical trials have been registered for this compound. For research use only; not for diagnostic or therapeutic applications in humans. |
| Molecular Formula |
C21H20O12
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|---|---|
| Molecular Weight |
464.38
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| Exact Mass |
464.095
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| CAS # |
145134-61-8
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| PubChem CID |
85469293
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| Appearance |
White to yellow solid powder
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| Density |
1.87±0.1 g/cm3(Predicted)
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| Boiling Point |
894.7±65.0 °C(Predicted)
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| LogP |
0.4
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| Hydrogen Bond Donor Count |
8
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
33
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| Complexity |
750
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| Defined Atom Stereocenter Count |
5
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| SMILES |
C1=CC(=CC=C1C2=C(C(=O)C3=C(O2)C=C(C(=C3O)O)O)O[C@H]4[C@@H]([C@H]([C@@H]([C@H](O4)CO)O)O)O)O
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| InChi Key |
DIYGQKBUNSAYQA-CZTZGLBASA-N
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| InChi Code |
InChI=1S/C21H20O12/c22-6-11-14(26)17(29)18(30)21(32-11)33-20-16(28)12-10(5-9(24)13(25)15(12)27)31-19(20)7-1-3-8(23)4-2-7/h1-5,11,14,17-18,21-27,29-30H,6H2/t11-,14-,17+,18-,21+/m1/s1
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| Chemical Name |
5,6,7-trihydroxy-2-(4-hydroxyphenyl)-3-[(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, avoid exposure to moisture. |
| 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) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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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 | 2.1534 mL | 10.7670 mL | 21.5341 mL | |
| 5 mM | 0.4307 mL | 2.1534 mL | 4.3068 mL | |
| 10 mM | 0.2153 mL | 1.0767 mL | 2.1534 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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