Ebastine
Based on 1 publication(s) in Google Scholar
Ebastine (LAS-W 090) is an orally active, second-generation histamine H1 receptor antagonist. Ebastine can be used for the symptoms of allergic rhinitis and chronic idiopathic urticaria research.
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- Pureza: 99.95%
- No. CAS: 90729-43-4
- Fòrmula: C32H39NO2
- Peso molecular:469.66
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) Ebastine
MoreVer todos los productos específicos de isoformas Histamine Receptor
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Actividad biológica
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H1 Receptor |
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Cell Line
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Type | Value | Description | References |
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| HeLa | IC50 |
9.56 μM
Compound: Ebastine
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Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
Inhibition of Ebolavirus glycoprotein/matrix protein VP40 entry in human HeLa cells after 4.5 hrs beta-lactamase reporter assay
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[PMID: 29624387] |
| Vero | CC50 |
15.42 μM
Compound: Ebastine
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Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
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10.1101/2020.03.20.999730 |
| Vero | IC50 |
6.92 μM
Compound: Ebastine
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Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
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10.1101/2020.03.20.999730 |
Ebastine (10-500 ng/mL; 24-48 hours) treatment significantly increases the proliferation of HFDPC[2].
Ebastine (10-500 ng/mL; 24-48 hours) treatment shows dose-dependent increases in Cyclin D1, Cyclin E1, and Cyclin A expression levels. And the expression levels of Cdk4, Cdk2, and Cdc2 are alos increased. Ebastine treatment elevates expression levels of phospho-AKT and phospho-p44/42 extracellular signal-regulated kinase[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human follicle dermal papilla cells (HFDPC)
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Concentration:10 ng/mL, 50 ng/mL, 100 ng/mL, 200 ng/mL, 500 ng/mL
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Incubation Time:24 hours, 48 hours
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Result:The proliferative activity in cells was significantly enhanced.
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Cell Line:Human follicle dermal papilla cells (HFDPC)
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Concentration:10 ng/mL, 50 ng/mL, 100 ng/mL, 200 ng/mL, 500 ng/mL
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Incubation Time:24 hours
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Result:The expression levels of cell-cycle regulatory proteins and an antiapoptotic protein were increased in HFDPC.
Following oral administration of [14C]Ebastine at a dose of 2 mg/kg, the plasma level reached the maximum (Cmax) of 102 ng eq./ml at 2 h and decreased monophasically with t1/2 of 3.9 h. At 20 mg/kg, a monophasic decrease is also observed with Cmax of 1110 ng eq./ml at 4 h and with t1/2 of 4.0 h[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 90729-43-4
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Appearance Solid
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Peso molecular 469.66
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Fòrmula C32H39NO2
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Color White to off-white
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SMILES
O=C(C1=CC=C(C(C)(C)C)C=C1)CCCN2CCC(OC(C3=CC=CC=C3)C4=CC=CC=C4)CC2
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Synonyms
LAS-W 090; RP64305
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
Solvente y solubilidad
Ethanol : 58.75 mg/mL (125.09 mM; Need ultrasonic)
DMSO : 8.33 mg/mL (17.74 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 0.83 mg/mL (1.77 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 0.83 mg/mL (1.77 mM); Clear solution
This protocol yields a clear solution of ≥ 0.83 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (8.3 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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.
Pureza y Documentación
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Ficha de datos (273 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
[1]. J Sastre. Ebastine in allergic rhinitis and chronic idiopathic urticarial. Allergy. 2008 Dec;63 Suppl 89:1-20. [Content Brief]
[2]. Fu-Ming Tsai, et al. Extracellular Signal-Regulated Kinase Mediates Ebastine-Induced Human Follicle Dermal Papilla Cell Proliferation. Biomed Res Int. 2019 Feb 11;2019:6360503. [Content Brief]
[3]. Fujii, et al. Absorption, distribution, metabolism and excretion of [14C]ebastine after a single administration in rats. Arzneimittelforschung. 1994 Apr;44(4):527-38. [Content Brief]
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO / Ethanol | 1 mM | 2.1292 mL | 10.6460 mL | 21.2920 mL | 53.2300 mL |
| 5 mM | 0.4258 mL | 2.1292 mL | 4.2584 mL | 10.6460 mL | |
| 10 mM | 0.2129 mL | 1.0646 mL | 2.1292 mL | 5.3230 mL | |
| 15 mM | 0.1419 mL | 0.7097 mL | 1.4195 mL | 3.5487 mL | |
| Ethanol | 20 mM | 0.1065 mL | 0.5323 mL | 1.0646 mL | 2.6615 mL |
| 25 mM | 0.0852 mL | 0.4258 mL | 0.8517 mL | 2.1292 mL | |
| 30 mM | 0.0710 mL | 0.3549 mL | 0.7097 mL | 1.7743 mL | |
| 40 mM | 0.0532 mL | 0.2661 mL | 0.5323 mL | 1.3307 mL | |
| 50 mM | 0.0426 mL | 0.2129 mL | 0.4258 mL | 1.0646 mL | |
| 60 mM | 0.0355 mL | 0.1774 mL | 0.3549 mL | 0.8872 mL | |
| 80 mM | 0.0266 mL | 0.1331 mL | 0.2661 mL | 0.6654 mL | |
| 100 mM | 0.0213 mL | 0.1065 mL | 0.2129 mL | 0.5323 mL |
Ebastine Related Classifications
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