| Size | Price | Stock | Qty |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Other Sizes |
| Targets |
MitoEbselen-2 targets mitochondria, where it acts as a glutathione peroxidase mimic to reduce lipid hydroperoxides. By catalyzing the reduction of these reactive oxygen species, it prevents oxidative damage to mitochondrial membranes and inhibits the activation of apoptotic pathways. Its mechanism involves the selenium atom in the ebselen moiety, which is essential for its peroxidase-like activity and radiation-mitigating properties.
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| ln Vitro |
At a concentration of 20 μM, MitoEbselen-2 chloride (5-20 μM; 30 min) affords ∼50% radioprotection/mitigation of mouse embryonic cells[1].
In vitro, MitoEbselen-2 functions as a potent antioxidant by reducing lipid hydroperoxides in mitochondrial membranes. It prevents apoptotic cell death induced by oxidative stress. Its activity has been demonstrated in cell-based assays where it protects cells from radiation-induced damage and oxidative injury. It is also effective in preventing apoptosis and lowering lipid hydroperoxides. |
| ln Vivo |
Mice exposed to whole-body γ-irradiation have a higher survival rate when mitoEbselen-2 chloride is administered (100 μL of 4 mg/mL; i.v.)[1].
In vivo, MitoEbselen-2 has been shown to act as a radiation mitigator. It extends the survival time of mice exposed to whole-body irradiation after 24 hours of radiation exposure. Its mitochondria-targeting property allows it to accumulate in mitochondria, where it effectively reduces oxidative damage and prevents cell death. These findings support its potential as a radioprotective agent. |
| Enzyme Assay |
The in vitro assay for MitoEbselen-2 typically measures its ability to reduce lipid hydroperoxides. These cell-free assays use purified mitochondrial membranes or liposomes containing lipid hydroperoxides and measure the reduction in hydroperoxide levels using colorimetric or fluorometric methods. Its glutathione peroxidase-like activity is assessed using standard peroxidase assays with a suitable substrate.
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| Cell Assay |
In vitro cellular assays for MitoEbselen-2 assess its cytoprotective and antioxidant effects. Cells are treated with MitoEbselen-2 and then exposed to oxidative stress or radiation. Cell viability, mitochondrial membrane potential, and markers of apoptosis (e.g., caspase-3 activation) are measured. Its ability to reduce lipid hydroperoxides in cells is also assessed using lipid peroxidation assays.
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| Animal Protocol |
In vivo animal studies for MitoEbselen-2 have been conducted in mouse models of whole-body irradiation. Mice are administered MitoEbselen-2 before or after radiation exposure, and survival is monitored. Other endpoints include tissue oxidative damage, apoptosis markers, and mitochondrial function. These studies demonstrate the compound's efficacy as a radiation mitigator.
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| ADME/Pharmacokinetics |
Specific pharmacokinetic data for MitoEbselen-2 are not extensively detailed in the available literature. As a mitochondria-targeted compound, it is expected to accumulate in mitochondria, where it exerts its antioxidant effects. Its pharmacokinetic properties would be important for its development as a radiation mitigator, but specific parameters such as half-life and bioavailability are not provided.
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| Toxicity/Toxicokinetics |
Specific toxicity data for MitoEbselen-2 are not extensively detailed in the available literature. As a mitochondria-targeted antioxidant, its toxicity profile is likely related to its mechanism of action. However, its efficacy in extending survival in irradiated mice suggests a favorable therapeutic index. It is intended for research purposes only and is not for human use.
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| References | |
| Additional Infomation |
MitoEbselen-2 (CAS 1638973-78-0), also known as MitoPeroxidase-2, is a mitochondria-targeted ebselen derivative and a glutathione peroxidase mimic. It acts as a potent radiation mitigator by reducing mitochondrial lipid hydroperoxides and preventing apoptotic cell death. It has been shown to extend the survival of mice exposed to whole-body irradiation. It is a research compound and is not approved for clinical use.
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| Molecular Formula |
C35H30CLN2O2PSE
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|---|---|
| Molecular Weight |
656.011667728424
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| Exact Mass |
656.089
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| Elemental Analysis |
C, 64.08; H, 4.61; Cl, 5.40; N, 4.27; O, 4.88; P, 4.72; Se, 12.04
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| CAS # |
1638973-78-0
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| Related CAS # |
1638973-78-0; 1639112-57-4 (cation);
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| PubChem CID |
154730924
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| Appearance |
Solid powder
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
9
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| Heavy Atom Count |
42
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| Complexity |
813
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)[P+](CCNC(=O)CC2=CC=C(C=C2)N3C(=O)C4=CC=CC=C4[Se]3)(C5=CC=CC=C5)C6=CC=CC=C6.[Cl-]
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| InChi Key |
RWZPPTYDYPSPOY-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C35H29N2O2PSe.ClH/c38-34(26-27-20-22-28(23-21-27)37-35(39)32-18-10-11-19-33(32)41-37)36-24-25-40(29-12-4-1-5-13-29,30-14-6-2-7-15-30)31-16-8-3-9-17-31;/h1-23H,24-26H2;1H
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| Chemical Name |
2-[[2-[4-(3-oxo-1,2-benzoselenazol-2-yl)phenyl]acetyl]amino]ethyl-triphenylphosphanium;chloride
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| Synonyms |
MitoEbselen 2; MitoPeroxidase 2; MitoEbselen-2; MitoPeroxidase-2
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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 |
| 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 | 1.5244 mL | 7.6218 mL | 15.2437 mL | |
| 5 mM | 0.3049 mL | 1.5244 mL | 3.0487 mL | |
| 10 mM | 0.1524 mL | 0.7622 mL | 1.5244 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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