| 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 Note: (1). This product requires protection from light (avoid light exposure) during transportation and storage. (2). Please store this product in a sealed and protected environment (e.g. under nitrogen), 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)
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| Solubility (In Vitro) |
DMSO: ~50 mg/mL (~76.2 mM; with ultrasonication)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (1.91 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 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 DMSO stock solution (12.5 mg/mL) to 400 μL of PEG300 and mix well; then add 50 μL of Tween-80 and mix well; finally add 450 μL of physiological saline and 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: 1.25 mg/mL (1.91 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), Suspended solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of DMSO stock solution (12.5 mg/mL) to 900 μL of 20% SBE-β-CD saline and mix well. 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. Solubility in Formulation 3: ≥ 1.25 mg/mL (1.91 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (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 DMSO stock solution (12.5 mg/mL) to 900 μL of corn oil and mix well. (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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