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Purity: ≥98%
Ebselen (formerly SPI-1005; PZ-51; DR-3305; CCG-39161), is an organoselenium-based small molecule biochemical compound with potential anti-inflammatory, anti-oxidant, and cytoprotective activity. It is a capsid inhibitor of HIV-1 replication and is also a voltage-dependent calcium channel (VDCC) blocker. Ebselen inhibits Mpro and COVID-19 virus with an IC50 of 0.67 μM and an EC50 of 4.67 μM, respectively. After oral gavage, Ebselen acts by mimicking the activity of glutathione peroxidase (GPx) and can utilize glutathione to reduce other unstable molecules, thus preventing the formation of reactive oxygen species (ROS) and reducing oxidative stress on the cell. In the cochlea, this agent may prevent drug-induced injury to the auditory hair cells thereby preventing hearing loss. GPx is the main antioxidant enzyme in the cochlea and protects the inner ear from loud sounds and biochemical damage. In addition, ebselen is able to inhibit the activity of many enzymes involved in inflammation.
| ln Vitro |
In COVID-19 virus-infected Vero cells, Ebselen (SPI-1005; 0.4-100 μM; 20-24 hours) exhibits potent antiviral effects at a concentration of 10 μM treatment. Ebsele attaches itself covalently to COVID-19 virus Mpro's catalytic dyad at position C145[3]. Viral postentry events of the HIV-1 life cycle are inhibited by ebselen through a decrease in the incoming capsid uncoating process[4]. In the mouse brain, endogenous inositol monophosphatase is inhibited by ebselen, which also penetrates the blood-brain barrier. Inositol monophosphatase (IMPase) is inhibited by ebselen [5]. Ebselen suppresses invasion of pancreatic and renal cancer cell lines and inhibits the enzymatic activity of QSOX1[6].
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| ln Vivo |
In a dose-dependent manner, ebselen (5, 10 mg/kg; IP) reduces head twitches induced by 5-HT2 agonists[5].
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| Cell Assay |
RT-PCR[3]
Cell Types: COVID-19 virus infected Vero cells Tested Concentrations: 0.4, 1.2, 3.7, 11.1, 33.3, 100 μM Incubation Duration: 20-24 hrs (hours) Experimental Results: demonstrated strong antiviral effects at a concentration of 10 μM treatment. |
| Animal Protocol |
Animal/Disease Models: 20-25 g 10-12 week old male C57Bl6 mice[5]
Doses: 5, 10 mg/kg Route of Administration: IP Experimental Results: diminished 5-HT2 agonist-induced head twitches in a dose-dependent manner. |
| References |
[1]. Liang Q, et al. Electrical Stimulation Degenerated Cochlear Synapses Through Oxidative Stress in NeonatalCochlear Explants. Front Neurosci. 2019 Oct 14;13:1073.
[2]. H Sies, et al. Ebselen, a Selenoorganic Compound as Glutathione Peroxidase Mimic [3]. Jin Z, et al. Structure of Mpro from COVID-19 virus and discovery of its inhibitors. Nature. 2020 Apr 9. [4]. Thenin-Houssier S, et al. Ebselen, a Small-Molecule Capsid Inhibitor of HIV-1 Replication. Antimicrob Agents Chemother. 2016 Mar 25;60(4):2195-208. [5]. Singh N, et al. A safe lithium mimetic for bipolar disorder. Nat Commun. 2013;4:1332. doi: 10.1038/ncomms2320. [6]. Hanavan PD, et al. Ebselen inhibits QSOX1 enzymatic activity and suppresses invasion of pancreatic and renal cancer cell lines. Oncotarget. 2015 Jul 30;6(21):18418-28. |
| Molecular Formula |
C₁₃H₉NOSE
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| Molecular Weight |
274.18
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| CAS # |
60940-34-3
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| Related CAS # |
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| SMILES |
O=C1N(C2=CC=CC=C2)[Se]C3=CC=CC=C13
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| 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) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (9.12 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 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 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to 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: ≥ 2.5 mg/mL (9.12 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 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 |
*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.
 Ebselen induces local structural changes in CA-CTD.Antimicrob Agents Chemother.2016 Mar 25;60(4):2195-208. |
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 Residues affected by ebselen in15N–labeled CA-CTD.Antimicrob Agents Chemother.2016 Mar 25;60(4):2195-208. |
 Mechanism of action of Ebselen.Antimicrob Agents Chemother.2016 Mar 25;60(4):2195-208. |
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