| Size | Price | Stock | Qty |
|---|---|---|---|
| 1mg |
|
||
| 5mg |
|
||
| Other Sizes |
| Targets |
15-LOX
Damnacanthol targets two distinct pathways involved in inflammation. First, it is an inhibitor of the 15-lipoxygenase (15-LOX) enzyme, which is involved in the production of pro-resolving and pro-inflammatory lipid mediators. Second, it inhibits the production of nitric oxide (NO) in activated macrophages, a key inflammatory signaling molecule. This dual activity makes it a valuable tool for studying inflammatory processes. |
|---|---|
| ln Vitro |
In vitro, Damnacanthol exhibits potent anti-15-lipoxygenase (15-LOX) activity. It has also been shown to inhibit nitric oxide (NO) production in LPS-activated RAW 264.7 macrophage cells. While a specific IC50 value for 15-LOX inhibition is not provided in the source, its activity has been confirmed in standard enzymatic assays. This compound is a valuable research tool for exploring the role of 15-LOX in the inflammatory response.
|
| ln Vivo |
In vivo activity data for Damnacanthol is not detailed in the provided sources. Based on its dual mechanism as a 15-LOX inhibitor and NO production inhibitor, it is hypothesized to have potential for treating inflammatory diseases. It could be evaluated in animal models such as LPS-induced endotoxemia to measure its effect on reducing serum NO and cytokine levels, or in models of chronic inflammation like collagen-induced arthritis. Formal in vivo studies would be needed.
|
| Enzyme Assay |
To assess 15-LOX inhibition, a cell-free enzyme assay is performed. Recombinant human 15-LOX-1 (or 15-LOX-2) is incubated in a reaction buffer with increasing concentrations of Damnacanthol (e.g., 1-100 uM). The reaction is started by adding the substrate linoleic acid. After a 5-10 minute incubation, the formation of the product (13-HPODE) is measured by the increase in absorbance at 234 nm using a spectrophotometer. The IC50 is calculated by comparing the activity of treated wells to that of the control.
|
| Cell Assay |
For NO inhibition assays, RAW 264.7 mouse macrophages are seeded in 96-well plates. The cells are pre-treated with various concentrations of Damnacanthol (e.g., 1-50 uM) for 1-2 hours. Inflammation is then induced by the addition of lipopolysaccharide (LPS, e.g., 1 ug/mL) and incubated for 24 hours. The cell supernatant is collected, and the concentration of nitrite (a stable breakdown product of NO) is measured using the Griess reagent assay. Cell viability is assessed via an MTT assay to differentiate between inhibition of NO production and cytotoxicity.
|
| Animal Protocol |
For in vivo studies, Damnacanthol could be tested in a mouse model of LPS-induced sepsis. Mice would be injected intraperitoneally with various doses of Damnacanthol (e.g., 5-50 mg/kg) formulated in a suitable vehicle (e.g., 10% DMSO in saline). One hour later, sepsis would be induced by an intraperitoneal injection of LPS (e.g., 10 mg/kg). Blood would be collected after 4-6 hours, and serum levels of nitrite (NO) and pro-inflammatory cytokines (TNF-alpha, IL-1beta, IL-6) would be measured by ELISA. This model would directly test the in vivo anti-inflammatory efficacy of the compound.
|
| ADME/Pharmacokinetics |
Detailed pharmacokinetic data for Damnacanthol is not publicly available. The compound has a molecular weight of 284.26 g/mol. For in vitro use, it is soluble in DMSO. For in vivo studies, a formulation of DMSO, PEG300, and saline is often used. Researchers would need to conduct pilot PK studies to determine its half-life, bioavailability, and plasma exposure in their specific animal model.
|
| Toxicity/Toxicokinetics |
Publicly available toxicology data for Damnacanthol is not detailed. In cell-based assays, concentrations up to 50 uM are typically used, and cytotoxicity is simultaneously assessed via an MTT or LDH assay. No specific toxicity data for primary mammalian cells is provided. For any animal study, a preliminary acute toxicity test to determine the maximum tolerated dose (MTD) is recommended. Standard safety precautions for handling chemical reagents apply.
|
| References |
|
| Additional Infomation |
Echinoyl alcohol has been reported to be found in Damnacanthus indicus, Damnacanthus major, and other organisms for which data is available.
Damnacanthol is a research-grade natural product and is not approved for clinical use. It is used primarily as a pharmacological tool to study the dual roles of 15-LOX and NO in inflammatory processes. As a natural anthraquinone from Noni, it is also a compound of interest for natural product chemistry and quality control of botanical extracts. The compound is typically stored at -20degC as a powder, protected from light and moisture. For research use only. |
| Molecular Formula |
C16H12O5
|
|---|---|
| Molecular Weight |
284.26
|
| Exact Mass |
284.068
|
| CAS # |
477-83-8
|
| PubChem CID |
160474
|
| Appearance |
Light yellow to yellow solid powder
|
| Density |
1.455g/cm3
|
| Boiling Point |
527.5ºC at 760mmHg
|
| Flash Point |
202ºC
|
| Vapour Pressure |
9.55E-12mmHg at 25°C
|
| Index of Refraction |
1.678
|
| LogP |
1.668
|
| Hydrogen Bond Donor Count |
2
|
| Hydrogen Bond Acceptor Count |
5
|
| Rotatable Bond Count |
2
|
| Heavy Atom Count |
21
|
| Complexity |
434
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
COC1=C2C(=CC(=C1CO)O)C(=O)C3=CC=CC=C3C2=O
|
| InChi Key |
ASFZQCLAQPBWDN-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C16H12O5/c1-21-16-11(7-17)12(18)6-10-13(16)15(20)9-5-3-2-4-8(9)14(10)19/h2-6,17-18H,7H2,1H3
|
| Chemical Name |
3-hydroxy-2-(hydroxymethyl)-1-methoxyanthracene-9,10-dione
|
| 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 | 3.5179 mL | 17.5895 mL | 35.1791 mL | |
| 5 mM | 0.7036 mL | 3.5179 mL | 7.0358 mL | |
| 10 mM | 0.3518 mL | 1.7590 mL | 3.5179 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
