Ebselen |
| رقم الكتالوجGC10331 |
إبسيلين (SPI-1005) ، محاكى الجلوتاثيون بيروكسيديز ، هو مانع قناة الكالسيوم (VDCC) الفعال المعتمد على الجهد
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 60940-34-3
Sample solution is provided at 25 µL, 10mM.
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Ebselen is a selenoorganic compound with glutathione peroxidase-like activity and is an anti-inflammatory and antioxidant agent[1]. Ebselen is an inhibitor of inositol monophosphatase (IMPase) with an IC50 of 1.5μM[2]. Ebselen is a potent scavenger of hydrogen peroxide and hydroperoxides, including membrane-bound phospholipid and cholesterol ester hydroperoxides[3]. Ebselen can penetrate the blood-brain barrier and has anti-inflammatory, antioxidant and anti-cancer activities[4].
In vitro, Ebselen (0-100μM) treatment of U266 and RPMI8226 cells for 24h reduced cell viability in a concentration-dependent manner, induced cell apoptosis, increased the generation of intracellular ROS, and induced the translocation of Bax protein from the cytosol to the mitochondria[5]. Ebselen (5-10μM) treatment of V79 cells reduced hydrogen peroxide-induced DNA damage[6]. Ebselen (10-20μM) inhibited the growth of A549 lung cancer cells, Calu-6 lung cancer cells and primary normal human lung fibroblasts (HPF) cells, with IC50 values of approximately 12.5μM, 10μM and 20μM, respectively[7].
In vivo, Ebselen (10mg/kg) was intraperitoneally injected into rats with spinal cord injury (SCI), which reduced the levels of malondialdehyde (MDA) and protein carbonyl (PC) in spinal cord tissue and prevented the inhibition of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px) and catalase (CAT) enzyme activities in tissues induced by SCI[8].
References:
[1] Nakamura Y, Feng Q, Kumagai T, et al. Ebselen, a glutathione peroxidase mimetic seleno-organic compound, as a multifunctional antioxidant: implication for inflammation-associated carcinogenesis[J]. Journal of Biological Chemistry, 2002, 277(4): 2687-2694.
[2] Ramli F F, Cowen P J, Godlewska B R. The potential use of ebselen in treatment-resistant depression[J]. Pharmaceuticals, 2022, 15(4): 485.
[3] Santofimia-Castaño P, Izquierdo-Alvarez A, de la Casa-Resino I, et al. Ebselen alters cellular oxidative status and induces endoplasmic reticulum stress in rat hippocampal astrocytes[J]. Toxicology, 2016, 357: 74-84.
[4] Ali F, Alom S, Ali S R, et al. Ebselen: A Review on its Synthesis, Derivatives, Anticancer Efficacy and Utility in Combating SARS-COV-2[J]. Mini Reviews in Medicinal Chemistry, 2024, 24(12): 1203-1225.
[5] Zhang L, Zhou L, Du J, et al. Induction of apoptosis in human multiple myeloma cell lines by ebselen via enhancing the endogenous reactive oxygen species production[J]. BioMed Research International, 2014, 2014(1): 696107.
[6] Miorelli S T, Rosa R M, Moura D J, et al. Antioxidant and anti-mutagenic effects of ebselen in yeast and in cultured mammalian V79 cells[J]. Mutagenesis, 2008, 23(2): 93-99.
[7] Park W H. Ebselen Inhibits the Growth of Lung Cancer Cells via Cell Cycle Arrest and Cell Death Accompanied by Glutathione Depletion[J]. Molecules, 2023, 28(18): 6472.
[8] Kalayci M, Coskun O, Cagavi F, et al. Neuroprotective effects of ebselen on experimental spinal cord injury in rats[J]. Neurochemical Research, 2005, 30: 403-410.
| Cell experiment [1]: | |
Cell lines | U266、RPMI8226 cells |
Preparation Method | Cells were treated with 0 (control), 10, 20, 30, 40, 50, and 100μM Ebselen for 24h, respectively. Concentration dependent changes of cell viability determined by CCK-8 assay in cells. |
Reaction Conditions | 0, 10, 20, 30, 40, 50, 100μM; 24h |
Applications | Ebselen induced a decrease in cell viability in a concentration-dependent manner. |
| Animal experiment [2]: | |
Animal models | Wistar albino rats |
Preparation Method | Rats were allotted in six experimental groups: A (control), B (only laminic tomy), C (Trauma; laminectomy+spinal trauma), D (Placebo group; laminectomy+spinal trauma+serum physiology), E (Methylprednisolone group; laminectomy+spinal trauma+Methylprednisolone treated), F (Ebselen group; laminectomy+spinal trauma+Ebselen treated), each containing six rats. Group A, B and C were not treated by any drug. Group D received 1 mL serum physiology, group E received 30mg/kg Methylprednisolone intraperitoneally (i.p.) and group F received 10mg/kg Ebselen i.p. just after the trauma. Rats were examined neurologically at 24h after trauma and spinal cord tissue samples were harvested for both biochemical and histopathological evaluation. |
Dosage form | 10mg/kg; i.p. |
Applications | Ebselen treatment reduced malondialdehyde (MDA) and protein carbonyl (PC) levels in spinal cord tissue and prevented SCI-induced inhibition of superoxide dismutase (SOD), glutathione peroxidase (GSH-Px), and catalase (CAT) enzyme activities in the tissue. |
References: | |
| Cas No. | 60940-34-3 | SDF | |
| Chemical Name | 2-phenylbenzo[d][1,2]selenazol-3(2H)-one | ||
| Canonical SMILES | O=C1C2=CC=CC=C2[Se]N1C3=CC=CC=C3 | ||
| Formula | C13H9NOSe | M.Wt | 274.18 |
| الذوبان | ≤5mg/ml in ethanol;5mg/ml in DMSO;5mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 3.6472 mL | 18.2362 mL | 36.4724 mL |
| 5 mM | 0.7294 mL | 3.6472 mL | 7.2945 mL |
| 10 mM | 0.3647 mL | 1.8236 mL | 3.6472 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid 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 master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
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3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: 99.97%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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