| Size | Price | Stock | Qty |
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| 2mg |
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| 5mg |
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| Other Sizes |
| Targets |
PI3K (phosphoinositide 3-kinase) isoforms α, β, γ, K, and δ (IC50=3.46-5.27 μM); tyrosine-specific protein kinase; phosphatidylinositol turnover. Orobol inhibits PI3K-mediated signaling pathways, which are involved in cell growth, survival, metabolism, and inflammation. It also shows antiviral effects against certain RNA and DNA viruses.
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| ln Vitro |
Orobol targets casein kinase 1 epsilon and binds to CK1ε in an ATP-competitive way to produce anti-obesity effects[2]. The phosphorylation of 4E-BP1 caused by MDI (isobutylmethylxanthine, dexamethasone, and insulin) is efficiently suppressed by orobol (5–20 μM)[2].
In vitro, Orobol inhibits PI3K isoforms with IC50 values of 3.46-5.27 μM. It exhibits antiviral effects against some animal viruses; addition of the compound after virus entry inhibits the appearance of late viral protein synthesis in Vesicular Stomatitis Virus, influenza, or vaccinia virus-infected cells, but has no effect on poliovirus protein synthesis. Orobol also shows anti-aging and anti-obesity effects in various cellular models. |
| ln Vivo |
In C57BL/6J mice, orobol reduces weight gain and lipid accumulation brought on by a high-fat diet without changing food intake[2].
In vivo activity data for Orobol are limited in the available literature. The compound's anti-obesity and anti-aging effects have been suggested based on in vitro studies, but comprehensive in vivo validation is lacking. Further studies in animal models would be needed to confirm its therapeutic potential and evaluate its pharmacokinetic properties and safety profile. |
| Enzyme Assay |
PI3K kinase activity is measured using a luminescent or radiometric kinase assay with recombinant PI3K isoforms (α, β, γ, δ, K) and a phosphatidylinositol substrate. The compound is incubated with the enzyme and ATP, and the IC50 values (3.46-5.27 μM) are determined by measuring product formation. Tyrosine-specific protein kinase inhibition is assessed using similar kinase assays with appropriate substrates.
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| Cell Assay |
Cells are treated with Orobol at varying concentrations for 24-72 hours. PI3K signaling is assessed by Western blot for phosphorylated AKT (Ser473) and other downstream effectors. Antiviral activity is evaluated by infecting cells with viruses (VSV, influenza, vaccinia, poliovirus) and measuring viral protein synthesis by Western blot or plaque assays. Cell viability is assessed using standard cytotoxicity assays.
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| Animal Protocol |
Animal/Disease Models: HFD-induced obesity in C57BL/6J mice[2]
Doses: 10 mg/kg Route of Administration: intragastrically (po); daily for 23 weeks Experimental Results: Dramatically diminished body weight by 17.3% compared to the HFD group. Specific in vivo protocols for Orobol are not well-documented. Potential studies could include high-fat diet-induced obesity models for evaluating anti-obesity effects, or viral infection models for assessing antiviral activity. The compound would be administered orally or intraperitoneally at doses determined from preliminary pharmacokinetic studies. Further research is needed to establish in vivo efficacy. |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Orobol is a known metabolite of genistein in the human body. Pharmacokinetic data for Orobol are not extensively characterized. The compound has molecular formula C15H10O6 and molecular weight 286.24. It is an isoflavone natural product with CAS number 480-23-9. Its oral bioavailability, half-life, and tissue distribution require further investigation. As a natural product, pharmacokinetic properties may vary depending on the formulation and route of administration. |
| Toxicity/Toxicokinetics |
No comprehensive toxicity data are currently available for Orobol. As a naturally occurring isoflavone, it is generally considered to have a favorable safety profile, but systematic toxicological evaluation is lacking. Standard preclinical toxicology studies would be necessary to establish its safety for potential therapeutic applications. For research use, standard laboratory safety precautions apply.
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| References | |
| Additional Infomation |
Orobol belongs to the class of 7-hydroxyisoflavones, which consists of isoflavones substituted with hydroxyl groups at the 5, 7, 3', and 4' positions. It has been isolated from the mycelium of Cordyceps sinensis. Orobol possesses dual activities including anti-inflammatory activity, free radical scavenging, and as both a plant and fungal metabolite. Its function is related to isoflavones. Orobol has also been reported to exist in Tritirachium, Flemingia macrophylla, and other organisms with relevant data.
Orobol (3',4',5,7-tetrahydroxyisoflavone) is a naturally occurring isoflavone found in various plant sources. It functions as a PI3K inhibitor (IC50=3.46-5.27 μM) with antiviral, anti-aging, and anti-obesity activities. It is a research tool for studying PI3K signaling, natural product pharmacology, and antiviral mechanisms. The compound has CAS number 480-23-9 and is supplied as a solid powder. It is for research use only and has not entered clinical trials or received FDA approval. |
| Molecular Formula |
C15H10O6
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|---|---|
| Molecular Weight |
286.24
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| Exact Mass |
286.047
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| CAS # |
480-23-9
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| PubChem CID |
5281801
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| Appearance |
White to off-white solid powder
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| Density |
1.7±0.1 g/cm3
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| Boiling Point |
616.1±55.0 °C at 760 mmHg
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| Flash Point |
239.5±25.0 °C
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| Vapour Pressure |
0.0±1.8 mmHg at 25°C
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| Index of Refraction |
1.768
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| LogP |
2.76
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
1
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| Heavy Atom Count |
21
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| Complexity |
447
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
IOYHCQBYQJQBSK-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C15H10O6/c16-8-4-12(19)14-13(5-8)21-6-9(15(14)20)7-1-2-10(17)11(18)3-7/h1-6,16-19H
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| Chemical Name |
3-(3,4-dihydroxyphenyl)-5,7-dihydroxychromen-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: This product requires protection from light (avoid light exposure) during transportation and storage. |
| 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 | 3.4936 mL | 17.4679 mL | 34.9357 mL | |
| 5 mM | 0.6987 mL | 3.4936 mL | 6.9871 mL | |
| 10 mM | 0.3494 mL | 1.7468 mL | 3.4936 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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