| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| Other Sizes |
| Targets |
Ebselen oxide targets multiple enzymes involved in oxidative stress and inflammation. It acts as a glutathione peroxidase mimetic, catalyzing the reduction of hydroperoxides. Ebselen oxide also inhibits thioredoxin reductase, an enzyme involved in redox regulation. By inhibiting these enzymes, ebselen oxide modulates cellular redox balance and reduces oxidative stress. The compound also inhibits lipoxygenases, which are involved in the production of inflammatory mediators.
|
|---|---|
| ln Vitro |
Ebselen oxide, is a covalent inhibitor of diguanylate cyclase (DGC) activity and c-di-GMP allosteric binding to I-site-containing proteins[1].
Ebselen oxide prevents the synthesis of c-di-GMP by diguanylate cyclase. Ebselen oxide exhibits increased potency on HDAC8 (IC50=0.2 μM) in comparison with Ebselen[3]. In vitro, Ebselen oxide has been shown to have potent antioxidant activity. It catalyzes the reduction of hydroperoxides, protecting cells from oxidative damage. The compound also inhibits thioredoxin reductase and lipoxygenases. Ebselen oxide has been shown to protect cells from oxidative stress-induced cell death. The compound's anti-inflammatory effects have been demonstrated in various in vitro models. |
| ln Vivo |
In vivo, Ebselen oxide has been studied in animal models of oxidative stress and inflammation. The compound has been shown to protect against ischemic injury, neurodegenerative diseases, and inflammation. Ebselen oxide has been shown to reduce infarct size in models of stroke and to protect against neuronal damage in models of Parkinson's disease. The compound's antioxidant and anti-inflammatory effects contribute to its protective effects in vivo.
|
| Enzyme Assay |
In vitro enzyme inhibition assays for Ebselen oxide typically involve measuring the activity of glutathione peroxidase, thioredoxin reductase, or lipoxygenases in the presence of varying concentrations of the compound. The enzyme is incubated with its substrate and Ebselen oxide, and the enzymatic activity is measured. The IC50 value for inhibition of the enzyme is determined from dose-response curves.
|
| Cell Assay |
In vitro cell-based studies with Ebselen oxide typically involve cultured cells, such as neurons, cardiomyocytes, or macrophages. Cells are treated with Ebselen oxide at various concentrations in the presence or absence of oxidative stress or inflammatory stimuli. Cell viability is assessed using MTT or similar assays. Oxidative stress markers, such as reactive oxygen species and lipid peroxidation, are measured. The effect of Ebselen oxide on inflammatory cytokine production is assessed by ELISA.
|
| Animal Protocol |
In vivo animal studies with Ebselen oxide are typically conducted in rodent models of oxidative stress and inflammation. The compound is administered orally or intraperitoneally. The effect of Ebselen oxide on infarct size in stroke models, on neuronal damage in neurodegenerative disease models, and on inflammation in inflammatory disease models is assessed. Pharmacokinetic studies are performed to evaluate the absorption and distribution of the compound.
|
| ADME/Pharmacokinetics |
The pharmacokinetic properties of Ebselen oxide have been studied in preclinical settings. Following oral administration, the compound is absorbed from the gastrointestinal tract. Ebselen oxide is metabolized in the liver. The elimination half-life is relatively short. Detailed PK parameters such as Cmax, Tmax, AUC, and half-life have been reported in the literature.
|
| Toxicity/Toxicokinetics |
The toxicity profile of Ebselen oxide has been evaluated in preclinical studies. The compound has been shown to have a relatively low toxicity in animal models at therapeutic doses. However, higher doses can cause adverse effects, including gastrointestinal upset and hepatotoxicity. The compound is for research use only and is not approved for human therapeutic use.
|
| References |
|
| Additional Infomation |
Ebselen oxide is a research compound with antioxidant, anti-inflammatory, and cytoprotective properties. It is used to study the role of oxidative stress and inflammation in various diseases, including stroke, neurodegenerative diseases, and inflammatory disorders. Ebselen oxide is not an FDA-approved drug and is not commercially available as a pharmaceutical product.
|
| Molecular Formula |
C13H9NO2SE
|
|---|---|
| Molecular Weight |
290.176062345505
|
| Exact Mass |
290.979
|
| Elemental Analysis |
C, 53.81; H, 3.13; N, 4.83; O, 11.03; Se, 27.21
|
| CAS # |
104473-83-8
|
| PubChem CID |
368655
|
| Appearance |
White to off-white solid powder
|
| Boiling Point |
277.3±23.0 °C at 760 mmHg
|
| Flash Point |
121.5±22.6 °C
|
| Vapour Pressure |
0.0±0.6 mmHg at 25°C
|
| LogP |
1.537
|
| Hydrogen Bond Donor Count |
0
|
| Hydrogen Bond Acceptor Count |
2
|
| Rotatable Bond Count |
1
|
| Heavy Atom Count |
17
|
| Complexity |
338
|
| Defined Atom Stereocenter Count |
0
|
| SMILES |
C1=CC=C(C=C1)N2C(=O)C3=CC=CC=C3[Se]2=O
|
| InChi Key |
SBTLFLABILGUMK-UHFFFAOYSA-N
|
| InChi Code |
InChI=1S/C13H9NO2Se/c15-13-11-8-4-5-9-12(11)17(16)14(13)10-6-2-1-3-7-10/h1-9H
|
| Chemical Name |
1-oxo-2-phenyl-1lambda4,2-benzoselenazol-3-one
|
| Synonyms |
Ebselen oxide
|
| 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: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| 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 | 3.4461 mL | 17.2307 mL | 34.4614 mL | |
| 5 mM | 0.6892 mL | 3.4461 mL | 6.8923 mL | |
| 10 mM | 0.3446 mL | 1.7231 mL | 3.4461 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.
|