| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
Uralenol targets protein tyrosine phosphatase 1B (PTP1B), a key negative regulator of insulin and leptin receptor signaling. PTP1B dephosphorylates the activated insulin receptor and its substrates, thereby attenuating insulin signal transduction. Uralenol also exhibits inhibitory activity against mushroom tyrosinase with an IC50 of 49.5 µM using L-tyrosine as substrate. Additionally, Uralenol shows affinity for estrogen and progestogen receptors, suggesting potential endocrine-modulating properties.
|
|---|---|
| ln Vitro |
In vitro, Uralenol exhibits potent PTP1B inhibitory activity with reported IC50 values of 21.5 µM. The compound significantly inhibits PTP1B enzyme activity in biochemical assays using purified enzyme preparations. Uralenol shows potent anti-proliferative effects on estrogen receptor-positive breast cancer MCF-7 cells in vitro. The compound also demonstrates inhibitory activity against mushroom tyrosinase, indicating potential applications in melanogenesis research.
|
| ln Vivo |
In vivo activity data for Uralenol are limited, as the compound is primarily used in cell-based and biochemical studies. Based on its PTP1B inhibitory mechanism, Uralenol is expected to enhance insulin signaling and improve glucose metabolism in animal models of diabetes and obesity. The compound's natural product origin and favorable bioactivity profile suggest potential for further in vivo evaluation. However, detailed pharmacokinetic and efficacy studies in animal models have not been extensively reported in the available literature.
|
| Enzyme Assay |
The in vitro enzyme inhibition assay for Uralenol typically involves measuring PTP1B activity using a synthetic substrate such as p-nitrophenyl phosphate (pNPP). Purified recombinant human PTP1B enzyme is incubated with varying concentrations of Uralenol (typically 0.1-100 µM) in assay buffer at 37°C for 10-15 minutes. The reaction is initiated by adding the substrate, and after incubation, the reaction is stopped with NaOH. Absorbance at 405 nm is measured, and IC50 values are calculated from dose-response curves.
|
| Cell Assay |
For in vitro cell-based assays, cells such as MCF-7 breast cancer cells or insulin-responsive cell lines are cultured in appropriate medium and treated with Uralenol at various concentrations (1-100 µM) for 24-72 hours. Cell viability is assessed using MTT or CCK-8 assays. PTP1B activity is measured in cell lysates using a phosphatase activity assay kit. Insulin signaling is evaluated by Western blot analysis of phosphorylated insulin receptor and Akt. Anti-proliferative effects are quantified by cell counting or colony formation assays.
|
| Animal Protocol |
In vivo animal studies for Uralenol have not been extensively reported in the literature. Based on the compound's mechanism as a PTP1B inhibitor, potential in vivo studies would involve administration to diabetic or obese mouse models via oral gavage or intraperitoneal injection at doses ranging from 1-50 mg/kg. Efficacy would be assessed by measuring blood glucose levels, insulin sensitivity, and glucose tolerance. Tissue samples would be collected for analysis of PTP1B activity and insulin signaling biomarkers.
|
| ADME/Pharmacokinetics |
Pharmacokinetic properties of Uralenol have not been fully characterized. As a natural flavonoid compound, Uralenol is expected to have moderate oral bioavailability, with absorption and distribution influenced by its physicochemical properties. The compound may undergo extensive first-pass metabolism in the liver, and its elimination half-life is likely to be relatively short. Detailed pharmacokinetic studies are needed to determine parameters such as Cmax, Tmax, AUC, and protein binding.
|
| Toxicity/Toxicokinetics |
Toxicological data for Uralenol are limited. As a natural product, the compound is generally considered to have low acute toxicity, but comprehensive toxicology studies have not been conducted. The compound's inhibitory effects on PTP1B and tyrosinase suggest a favorable safety profile, but potential off-target effects and chronic toxicity remain to be evaluated. Standard in vitro toxicity assays such as Ames test, micronucleus test, and cytotoxicity screens should be performed for safety assessment.
|
| References | |
| Additional Infomation |
Uralenol is a type of flavonoid. It has been reported that ursenoyl exists in Broussonetia papyrifera, and relevant data are available for reference.
Uralenol is a natural PTP1B inhibitor from Broussonetia papyrifera with potential applications in diabetes and cancer research. The compound's ability to inhibit PTP1B, a validated target for type 2 diabetes and obesity, makes it a valuable tool for studying insulin signaling and metabolic regulation. Uralenol also shows anti-proliferative effects on breast cancer cells, suggesting potential anticancer applications. The compound is intended for research use only and is not approved for therapeutic use. |
| Molecular Formula |
C20H18O7
|
|---|---|
| Molecular Weight |
370.35
|
| Exact Mass |
370.105
|
| CAS # |
139163-15-8
|
| PubChem CID |
5315126
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.519g/cm3
|
| Boiling Point |
654.1ºC at 760 mmHg
|
| Melting Point |
170.5 - 172.5 °C
|
| Flash Point |
236.6ºC
|
| Vapour Pressure |
1.04E-17mmHg at 25°C
|
| Index of Refraction |
1.723
|
| LogP |
3.496
|
| Hydrogen Bond Donor Count |
5
|
| Hydrogen Bond Acceptor Count |
7
|
| Rotatable Bond Count |
3
|
| Heavy Atom Count |
27
|
| Complexity |
636
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
CC(=CCC1=C(C(=CC(=C1)C2=C(C(=O)C3=C(C=C(C=C3O2)O)O)O)O)O)C
|
| InChi Key |
WOMWVGHYSNATOB-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C20H18O7/c1-9(2)3-4-10-5-11(6-14(23)17(10)24)20-19(26)18(25)16-13(22)7-12(21)8-15(16)27-20/h3,5-8,21-24,26H,4H2,1-2H3
|
| Chemical Name |
2-[3,4-dihydroxy-5-(3-methylbut-2-enyl)phenyl]-3,5,7-trihydroxychromen-4-one
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| 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
|
|---|---|
| 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 | 2.7001 mL | 13.5007 mL | 27.0015 mL | |
| 5 mM | 0.5400 mL | 2.7001 mL | 5.4003 mL | |
| 10 mM | 0.2700 mL | 1.3501 mL | 2.7001 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.