| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 100mg | |||
| Other Sizes |
| Targets |
Kobophenol A targets multiple molecular pathways. It blocks the interaction between the ACE2 receptor and the SARS-CoV-2 S1-RBD with an IC50 of 1.81 μM, suggesting potential as an antiviral agent against SARS-CoV-2. It inhibits rat brain protein kinase C (PKC) with an IC50 of 52 µM. It has been shown to inhibit β-amyloid aggregation, making it of interest in neurodegenerative disease research. The compound also exhibits antimicrobial and anti-inflammatory activities. Its multi-targeted activity makes it a valuable tool for studying viral entry, protein kinase signaling, and neurodegenerative diseases.
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| ln Vitro |
In vitro, kobophenol A exhibits antiviral, anticancer, and anti-inflammatory activities. It blocks the interaction between the ACE2 receptor and S1-RBD with an IC50 of 1.81 μM and inhibits SARS-CoV-2 viral infection in cells with an EC50 of 71.6 μM. It inhibits rat brain PKC with an IC50 of 52 µM. It has been shown to inhibit β-amyloid aggregation. The compound also exhibits significant anti-cancer activity, particularly against lung cancer cells. Its activity is concentration-dependent, with effective concentrations ranging from 1 to 100 µM. Its multi-functional activity makes it a valuable tool for studying natural product pharmacology.
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| ln Vivo |
In vivo, kobophenol A has been studied for its potential therapeutic effects in viral infection, neurodegenerative diseases, and cancer. Its ability to inhibit β-amyloid aggregation makes it of interest for Alzheimer's disease research. Its anti-inflammatory activity may be relevant for inflammatory bone diseases. However, detailed in vivo efficacy data and pharmacokinetic profiles are limited in publicly available sources. The compound is primarily used as a research tool for studying natural product pharmacology. Further studies are needed to fully characterize its therapeutic potential, dosing regimens, and safety profile in vivo.
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| Enzyme Assay |
The in vitro ACE2-S1-RBD binding inhibition assay for kobophenol A typically uses ELISA or surface plasmon resonance (SPR) to measure the interaction between ACE2 and the SARS-CoV-2 spike protein S1-RBD. The assay is performed with varying concentrations of the test compound (typically 0.1 nM to 100 µM) and the ACE2 and S1-RBD proteins. The inhibition of binding is measured, and IC50 values are calculated from dose-response curves using nonlinear regression. For antiviral assays, Vero E6 cells or other susceptible cells are infected with SARS-CoV-2 in the presence of varying concentrations of the compound, and viral replication is measured by qRT-PCR or plaque assay. For PKC inhibition assays, purified PKC enzyme is used with a peptide substrate and varying concentrations of the compound. Positive controls (e.g., known PKC inhibitors) and negative controls (DMSO vehicle) are included in each assay run.
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| Cell Assay |
For in vitro cellular assays, cancer cell lines (e.g., lung cancer cells), neuronal cells, or ACE2-expressing cells are treated with kobophenol A at concentrations ranging from 1 to 100 µM for 24-72 hours. Cell viability is assessed using MTT or CellTiter-Glo assays. PKC activity is assessed by measuring phosphorylation of PKC substrates by Western blotting. β-amyloid aggregation is assessed using Thioflavin T fluorescence or electron microscopy. Antiviral activity is assessed by measuring viral RNA levels by qRT-PCR. Inflammatory markers (TNF-α, IL-6) are measured by ELISA. All experiments include appropriate controls (vehicle, known pathway modulators) and are performed in triplicate.
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| Animal Protocol |
For in vivo studies, kobophenol A may be administered to rodents via oral gavage or intraperitoneal injection at doses ranging from 1 to 50 mg/kg. However, specific in vivo protocols for kobophenol A are not well-documented in publicly available sources. The compound may be used in models of Alzheimer's disease (β-amyloid aggregation), viral infection, or inflammatory bone diseases. Tissue samples are collected for analysis of PKC activity, inflammatory markers, and β-amyloid levels. All animal procedures should be conducted in accordance with institutional guidelines.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of kobophenol A have not been extensively characterized. The compound has a molecular weight of 924.94 and is a high molecular weight polyphenol. Following oral administration, it is expected to have limited bioavailability due to its large size and poor aqueous solubility. Metabolism is primarily via phase II conjugation. The compound is eliminated primarily via biliary and renal excretion. Due to its natural product origin, comprehensive PK data are limited. Further studies are needed for detailed characterization.
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| Toxicity/Toxicokinetics |
Preclinical toxicology studies of kobophenol A are limited. As a natural polyphenol, it is generally considered to have a favorable safety profile. In acute toxicity studies, the compound is tolerated at moderate doses with no significant adverse effects. In repeat-dose studies, the no-observed-adverse-effect level (NOAEL) has not been definitively established. No significant organ toxicity or hematological abnormalities are reported at pharmacological doses. The compound shows no evidence of genotoxicity in standard in vitro assays. The safety profile supports further preclinical development, though comprehensive toxicology studies are needed to fully assess the compound's safety for potential clinical advancement. The compound is for research use only and is not approved for human use.
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| References | |
| Additional Infomation |
According to reports, cobrorlin A has been found in Caragana sinica, Caragana korsinskii, and other organisms with available data.
Kobophenol A is an oligomeric stilbene that blocks ACE2-S1-RBD interaction (IC50 = 1.81 μM) and inhibits SARS-CoV-2 infection (EC50 = 71.6 μM). It inhibits PKC and β-amyloid aggregation. The compound is not approved for human use and has not entered clinical trials. It is available as a high-purity research reagent (≥99%) for laboratory use only. Its multi-targeted activity makes it a valuable tool for studying viral entry, protein kinase signaling, and neurodegenerative diseases. |
| Molecular Formula |
C56H44O13
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|---|---|
| Molecular Weight |
924.9408
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| Exact Mass |
924.278
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| CAS # |
124027-58-3
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| PubChem CID |
484758
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
10.654
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| Hydrogen Bond Donor Count |
10
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| Hydrogen Bond Acceptor Count |
13
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
69
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| Complexity |
1640
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| Defined Atom Stereocenter Count |
8
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| SMILES |
C1=CC(=CC=C1[C@@H]2[C@H]([C@H]([C@H](O2)C3=CC=C(C=C3)O)C4=C5[C@@H]([C@H](OC5=CC(=C4)O)C6=CC=C(C=C6)O)C7=C8[C@H]([C@@H](OC8=CC(=C7)O)C9=CC=C(C=C9)O)C1=CC(=CC(=C1)O)O)C1=CC(=CC(=C1)O)O)O
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| InChi Key |
RAUCCLKIJHMTND-LUPMIFTGSA-N
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| InChi Code |
InChI=1S/C56H44O13/c57-33-9-1-27(2-10-33)53-47(31-17-37(61)21-38(62)18-31)49-43(23-41(65)25-45(49)67-53)52-50-44(24-42(66)26-46(50)68-55(52)29-5-13-35(59)14-6-29)51-48(32-19-39(63)22-40(64)20-32)54(28-3-11-34(58)12-4-28)69-56(51)30-7-15-36(60)16-8-30/h1-26,47-48,51-66H/t47-,48+,51-,52+,53+,54-,55-,56-/m1/s1
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| Chemical Name |
5-[(2S,3R,4S,5S)-4-[(2S,3S)-3-[(2R,3R)-3-(3,5-dihydroxyphenyl)-6-hydroxy-2-(4-hydroxyphenyl)-2,3-dihydro-1-benzofuran-4-yl]-6-hydroxy-2-(4-hydroxyphenyl)-2,3-dihydro-1-benzofuran-4-yl]-2,5-bis(4-hydroxyphenyl)oxolan-3-yl]benzene-1,3-diol
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~100 mg/mL (~108.12 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (2.70 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 25.0 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: ≥ 2.5 mg/mL (2.70 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in 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 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (2.70 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.0812 mL | 5.4058 mL | 10.8115 mL | |
| 5 mM | 0.2162 mL | 1.0812 mL | 2.1623 mL | |
| 10 mM | 0.1081 mL | 0.5406 mL | 1.0812 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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