Ebselen (SPI-1005), a glutathione peroxidase mimetic, is a potent voltage-dependent calcium channel (VDCC) blocker. Ebselen potently inhibits Mpro (IC50=0.67 μM) and COVID-19 virus (EC50=4.67 μM).Ebselen is an inhibitor of HIV-1 capsid CTD dimerization. Ebselen, an organoselenium compound, can permeate the blood-brain barrier and has anti-inflammatory, antioxidant and anticancer activity.
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Ebselen Chemische Struktur
CAS. Nr. : 60940-34-3
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Ebselen influences the expression of apoptosis‑related proteins. The effects of ebselen on C‑Caspase‑8, C‑Caspase‑3, Bax, Bcl‑2 and C‑PARP are analyzed by western blotting.
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Beschreibung
Ebselen (SPI-1005), a glutathione peroxidase mimetic, is a potent voltage-dependent calcium channel (VDCC) blocker[1][2]. Ebselen potently inhibits Mpro (IC50=0.67 μM) and COVID-19 virus (EC50=4.67 μM)[3].Ebselen is an inhibitor of HIV-1 capsid CTD dimerization. Ebselen, an organoselenium compound, can permeate the blood-brain barrier and has anti-inflammatory, antioxidant and anticancer activity[4][5].
IC50 & Target
HIV-1
In Vitro
Ebselen (SPI-1005; 0.4-100 μM; 20-24 hours) shows strong antiviral effects at a concentration of 10 μM treatment in COVID-19 virus infected Vero cells. Ebsele covalently binds to C145 of the catalytic dyad in COVID-19 virus Mpro[3]. ?
Ebselen inhibits early viral postentry events of the HIV-1 life cycle by impairing the incoming capsid uncoating process[4]. ?
Ebselen permeates the blood-brain barrier and inhibits endogenous inositol monophosphatase in mouse brain. Ebselen inhibits inositol monophosphatase (IMPase)[5]. ?
Ebselen inhibits QSOX1 enzymatic activity and suppresses invasion of pancreatic, renal cancer cell lines[6].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Ebselen Related Antibodies
RT-PCR[3]
Cell Line:
COVID-19 virus infected Vero cells
Concentration:
0.4, 1.2, 3.7, 11.1, 33.3, 100 μM
Incubation Time:
20-24 hours
Result:
Showed strong antiviral effects at a concentration of 10 μM treatment.
In Vivo
Ebselen (5, 10 mg/kg; IP) decreases 5-HT2 agonist-induced head twitches in a dose-dependent manner[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model:
20-25 g 10-12 week old male C57Bl6 mice[5]
Dosage:
5, 10 mg/kg
Administration:
IP
Result:
Decreased 5-HT2 agonist-induced head twitches in a dose-dependent manner.
Klinische Studie
Molekulargewicht
274.18
Formel
C13H9NOSe
CAS. Nr.
60940-34-3
Appearance
Solid
Color
Light yellow to yellow
SMILES
O=C1N(C2=CC=CC=C2)[Se]C3=C1C=CC=C3
Versand
Room temperature in continental US; may vary elsewhere.
Speicherung
Powder
-20°C
3 years
4°C
2 years
In solvent
-80°C
1 year
-20°C
6 months
Lösungsmittel & Löslichkeit
In Vitro:
DMSO : 50 mg/mL (182.36 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Preparing Stock Solutions
ConcentrationSolventMass
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
View the Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day. The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Protocol 1
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2
Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (9.12 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μLDMSO stock solution (25.0 mg/mL) to 900 μLCorn oil, and mix evenly.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
Dosage
mg/kg
Animal weight (per animal)
g
Dosing volume (per animal)
μL
Number of animals
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO+
%
+
%
Tween-80
+
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO,
. All of co-solvents are available by MedChemExpress (MCE).
, Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration:
mg/mL
Method for preparing stock solution:
mg
drug dissolved in
μL
DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take
μL DMSO stock solution, add
μL .
μL , mix evenly, next add
μL Tween 80, mix evenly, then add
μL Saline.
Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution
If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
[1]. Liang Q, et al. Electrical Stimulation Degenerated Cochlear Synapses Through Oxidative Stress in NeonatalCochlear Explants. Front Neurosci. 2019 Oct 14;13:1073.
[Content Brief]
[2]. H Sies, et al. Ebselen, a Selenoorganic Compound as Glutathione Peroxidase Mimic
[Content Brief]
[3]. Jin Z, et al. Structure of Mpro from COVID-19 virus and discovery of its inhibitors. Nature. 2020 Apr 9.
[Content Brief]
[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.
[Content Brief]
[5]. Singh N, et al. A safe lithium mimetic for bipolar disorder. Nat Commun. 2013;4:1332. doi: 10.1038/ncomms2320.
[Content Brief]
[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.
[Content Brief]
[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.
Complete Stock Solution Preparation Table
*Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles. Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.
Optional Solvent
ConcentrationSolventMass
1 mg
5 mg
10 mg
25 mg
DMSO
1 mM
3.6472 mL
18.2362 mL
36.4724 mL
91.1810 mL
5 mM
0.7294 mL
3.6472 mL
7.2945 mL
18.2362 mL
10 mM
0.3647 mL
1.8236 mL
3.6472 mL
9.1181 mL
15 mM
0.2431 mL
1.2157 mL
2.4315 mL
6.0787 mL
20 mM
0.1824 mL
0.9118 mL
1.8236 mL
4.5590 mL
25 mM
0.1459 mL
0.7294 mL
1.4589 mL
3.6472 mL
30 mM
0.1216 mL
0.6079 mL
1.2157 mL
3.0394 mL
40 mM
0.0912 mL
0.4559 mL
0.9118 mL
2.2795 mL
50 mM
0.0729 mL
0.3647 mL
0.7294 mL
1.8236 mL
60 mM
0.0608 mL
0.3039 mL
0.6079 mL
1.5197 mL
80 mM
0.0456 mL
0.2280 mL
0.4559 mL
1.1398 mL
100 mM
0.0365 mL
0.1824 mL
0.3647 mL
0.9118 mL
Ebselen Related Classifications
Help & FAQs
Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.
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