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| 5mg |
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| Targets |
Episappanol targets pro-inflammatory cytokines, particularly interleukin-6 (IL-6) and tumor necrosis factor-alpha (TNF-α). By inhibiting the secretion of these cytokines, the compound exerts anti-inflammatory effects. The compound is a natural homoisoflavonoid and has been studied for its ability to scavenge free radicals, inhibit inflammatory mediators, and protect neuronal cells from oxidative stress.
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| ln Vitro |
In cell-free biochemical systems, Episappanol has been studied for its ability to scavenge free radicals. The compound's anti-inflammatory activity is primarily evaluated in cell-based systems by measuring its inhibition of IL-6 and TNF-α secretion. It also shows potential anticancer properties by inducing apoptosis in certain cancer cell lines.
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| ln Vivo |
In cell-based assays, Episappanol significantly inhibits the secretion of pro-inflammatory cytokines IL-6 and TNF-α. The compound has anti-inflammatory activity and can protect neuronal cells from oxidative stress. It also shows potential anticancer properties by inducing apoptosis in certain cancer cell lines. The compound's effects on cytokine production and cell viability are evaluated in various cell lines.
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| Enzyme Assay |
The cell-free assay for Episappanol involves measuring its free radical scavenging activity. This can be assessed using DPPH (2,2-diphenyl-1-picrylhydrazyl) or ABTS (2,2'-azino-bis(3-ethylbenzothiazoline-6-sulfonic acid)) assays. The compound's ability to inhibit inflammatory mediators can be evaluated in cell-free systems by measuring its effects on purified enzymes or signaling proteins.
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| Cell Assay |
Cell-based assays for Episappanol involve culturing immune cells such as macrophages and treating them with the compound at concentrations ranging from 0.1 to 100 μM. Cells are stimulated with LPS to induce cytokine production. IL-6 and TNF-α levels in the supernatant are measured by ELISA. The compound's anti-inflammatory effects are assessed by measuring the inhibition of cytokine secretion. Neuronal cells are used to assess protection from oxidative stress.
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| Animal Protocol |
There is no established animal experimental protocol for Episappanol specifically. As an anti-inflammatory natural product, the compound could potentially be evaluated in animal models of inflammation. Typical studies involve administration of the compound to mice via oral or intraperitoneal routes. Inflammatory markers and tissue damage are assessed in models of acute or chronic inflammation.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of Episappanol have not been extensively reported. As a small molecule with a molecular weight of 304.29 g/mol, the compound would be expected to have moderate oral bioavailability and tissue penetration. The compound is soluble in DMSO. Further pharmacokinetic studies would be required to determine plasma half-life, clearance, and metabolic pathways.
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| Toxicity/Toxicokinetics |
Episappanol is intended for research use only and lacks established toxicity profiles for therapeutic applications. Standard laboratory safety precautions should be observed when handling this natural product. As an anti-inflammatory compound, it may have effects on immune function. Standard toxicity studies in rodents would be required to determine the safety profile if therapeutic development is pursued.
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| References | |
| Additional Infomation |
There have been reports of Episappanol being found in Biancaea decapetala, and relevant data is available for reference.
Episappanol is a research-grade natural product supplied for anti-inflammatory and cancer research. It is not an approved pharmaceutical and has no clinical trial history. The compound is a natural homoisoflavonoid isolated from Caesalpinia sappan heartwood. It has anti-inflammatory activity and inhibits IL-6 and TNF-α secretion. This product is intended for research use only and is not for human therapeutic applications. |
| Molecular Formula |
C16H16O6
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|---|---|
| Molecular Weight |
304.29
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| Exact Mass |
304.094
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| CAS # |
111254-18-3
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| PubChem CID |
13846650
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| Appearance |
Off-white to pink solid powder
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| Density |
1.6±0.1 g/cm3
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| Boiling Point |
583.1±50.0 °C at 760 mmHg
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| Flash Point |
306.5±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.740
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| LogP |
0.85
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
22
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| Complexity |
391
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| Defined Atom Stereocenter Count |
2
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| SMILES |
C1[C@@]([C@@H](C2=C(O1)C=C(C=C2)O)O)(CC3=CC(=C(C=C3)O)O)O
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| InChi Key |
MPGFEHZDABUJFR-HZPDHXFCSA-N
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| InChi Code |
InChI=1S/C16H16O6/c17-10-2-3-11-14(6-10)22-8-16(21,15(11)20)7-9-1-4-12(18)13(19)5-9/h1-6,15,17-21H,7-8H2/t15-,16-/m1/s1
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| Chemical Name |
(3R,4R)-3-[(3,4-dihydroxyphenyl)methyl]-2,4-dihydrochromene-3,4,7-triol
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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 | 3.2863 mL | 16.4317 mL | 32.8634 mL | |
| 5 mM | 0.6573 mL | 3.2863 mL | 6.5727 mL | |
| 10 mM | 0.3286 mL | 1.6432 mL | 3.2863 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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