| Size | Price | Stock | Qty |
|---|---|---|---|
| 100mg |
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| 250mg | |||
| Other Sizes |
| Targets |
4',5-Dihydroxyflavone targets two key enzymes: soybean lipoxygenase-1 (LOX-1) and yeast α-glucosidase. It acts as a non-competitive or competitive inhibitor of these enzymes, with a Ki of 102.6 μM for soybean LOX-1 and an IC₅₀ of 66 μM for yeast α-glucosidase.
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|---|---|
| ln Vitro |
In vitro, 4',5-Dihydroxyflavone is a potent inhibitor of soybean LOX-1 (Ki = 102.6 μM) and yeast α-glucosidase (IC₅₀ = 66 μM). This dual inhibitory activity makes it a useful tool for studying both inflammatory pathways (via LOX inhibition) and carbohydrate metabolism (via α-glucosidase inhibition).
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| ln Vivo |
In vivo, the α-glucosidase inhibitory activity of 4',5-Dihydroxyflavone suggests potential applications in managing postprandial blood glucose levels, similar to other α-glucosidase inhibitors used for type 2 diabetes. However, its in vivo efficacy and safety have not been extensively studied.
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| Enzyme Assay |
In vitro non-cell enzyme assays for 4',5-Dihydroxyflavone involve measuring the inhibition of soybean LOX-1 activity using a spectrophotometric assay that monitors the formation of conjugated dienes from linoleic acid. α-Glucosidase inhibition is measured using a chromogenic substrate (e.g., p-nitrophenyl-α-D-glucopyranoside), and the release of p-nitrophenol is monitored.
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| Cell Assay |
In vitro cell-based assays for 4',5-Dihydroxyflavone use cell lines to study its effects on inflammation and glucose metabolism. For anti-inflammatory activity, macrophages are treated with the compound and stimulated with LPS, and the production of inflammatory mediators (e.g., leukotrienes) is measured. For anti-diabetic activity, intestinal epithelial cells (e.g., Caco-2) are used to study the inhibition of glucose uptake.
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| Animal Protocol |
In vivo animal studies for 4',5-Dihydroxyflavone would likely involve oral glucose tolerance tests (OGTT) in rodent models of diabetes to assess its ability to reduce postprandial blood glucose levels. Its anti-inflammatory effects could be studied in models of acute inflammation, such as carrageenan-induced paw edema.
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| ADME/Pharmacokinetics |
4',5-Dihydroxyflavone has a molecular weight of 254.24 g/mol and a molecular formula of C₁₅H₁₀O₄. It is a flavonoid with a purity of ≥98%. Detailed pharmacokinetic parameters, such as oral bioavailability, have not been extensively characterized.
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| Toxicity/Toxicokinetics |
The toxicity profile of 4',5-Dihydroxyflavone has not been fully characterized. As a flavonoid, it is generally considered to have low toxicity. However, comprehensive toxicological studies are needed.
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| References | |
| Additional Infomation |
4',5-Dihydroxyflavone is a flavonoid analog that inhibits soybean LOX-1 and yeast α-glucosidase. It is a valuable research tool for studying inflammation and carbohydrate metabolism. Also known as 5,4'-Dihydroxyflavone. Not approved for clinical use.
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| Molecular Formula |
C15H10O4
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|---|---|
| Molecular Weight |
254.2375
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| Exact Mass |
254.057
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| CAS # |
6665-67-4
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| PubChem CID |
165521
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| Appearance |
Light yellow to yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Boiling Point |
486.0±45.0 °C at 760 mmHg
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| Melting Point |
239-240ºC
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| Flash Point |
190.0±22.2 °C
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| Vapour Pressure |
0.0±1.3 mmHg at 25°C
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| Index of Refraction |
1.699
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| LogP |
2.32
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
19
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| Complexity |
382
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
OKRNDQLCMXUCGG-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10O4/c16-10-6-4-9(5-7-10)14-8-12(18)15-11(17)2-1-3-13(15)19-14/h1-8,16-17H
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| Chemical Name |
5-hydroxy-2-(4-hydroxyphenyl)chromen-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 |
| 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 : ≥ 155 mg/mL (~609.66 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.58 mg/mL (10.15 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 25.8 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: ≥ 2.58 mg/mL (10.15 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 25.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.9333 mL | 19.6665 mL | 39.3329 mL | |
| 5 mM | 0.7867 mL | 3.9333 mL | 7.8666 mL | |
| 10 mM | 0.3933 mL | 1.9666 mL | 3.9333 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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