Art. -Nr.: HY-B0674

Ebastine

(Synonyms: LAS-W 090; RP64305)

1 Cited Publications

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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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Reinheit: 99.95%
CAS. Nr.: 90729-43-4
Formel: C₃₂H₃₉NO₂
Molecular Weight:469.66

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Ebastine Chemical Structure

CAS. Nr.: 90729-43-4

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

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^[1].

IC₅₀ & Target^[1]

H₁ Receptor

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HeLa	IC₅₀	9.56 μM Compound: Ebastine	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	[PMID: 29624387]
Vero	CC₅₀	15.42 μM Compound: Ebastine	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	10.1101/2020.03.20.999730
Vero	IC₅₀	6.92 μM Compound: Ebastine	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	10.1101/2020.03.20.999730

In Vitro

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.

Cell Proliferation Assay^[2]

Cell Line:

Human follicle dermal papilla cells (HFDPC)
Concentration:

10 ng/mL, 50 ng/mL, 100 ng/mL, 200 ng/mL, 500 ng/mL
Incubation Time:

24 hours, 48 hours
Result:

The proliferative activity in cells was significantly enhanced.

Western Blot Analysis^[2]

Cell Line:

Human follicle dermal papilla cells (HFDPC)
Concentration:

10 ng/mL, 50 ng/mL, 100 ng/mL, 200 ng/mL, 500 ng/mL
Incubation Time:

24 hours
Result:

The expression levels of cell-cycle regulatory proteins and an antiapoptotic protein were increased in HFDPC.

In Vivo

In rats, after intravenous administration of [¹⁴C]Ebastine at 2 mg/kg, the plasma level of radioactivity decreased biphasically with α-phase half-life (t_1/2 α) of 1.6 h and β-phase half-life (t_1/2 β) of 3.1 h^[3].
Following oral administration of [¹⁴C]Ebastine at a dose of 2 mg/kg, the plasma level reached the maximum (C_max) of 102 ng eq./ml at 2 h and decreased monophasically with t_1/2 of 3.9 h. At 20 mg/kg, a monophasic decrease is also observed with C_max of 1110 ng eq./ml at 4 h and with t_1/2 of 4.0 h^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 90729-43-4
Appearance Solid
Molecular Weight 469.66
Formel C₃₂H₃₉NO₂
Color White to off-white
SMILES

O=C(C1=CC=C(C(C)(C)C)C=C1)CCCN2CCC(OC(C3=CC=CC=C3)C4=CC=CC=C4)CC2
Synonyms

LAS-W 090; RP64305
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

bioRxiv

2020 Jun.

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.1292 mL

10.6460 mL

21.2920 mL

5 mM

0.4258 mL

2.1292 mL

4.2584 mL

10 mM

0.2129 mL

1.0646 mL

2.1292 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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: ≥ 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.

Protocol 2

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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 0.83 mg/mL (1.77 mM); Clear solution

This protocol yields a clear solution of ≥ 0.83 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 μL DMSO stock solution (8.3 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

Keywords

Ebastine

1 Cited Publications

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Ebastine

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Publications Citing Use of MedChemExpress (MCE) Ebastine

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ebastine

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Neuronal Signaling Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

Neurotransmitter Receptor Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Parkinson's Disease Compound Library

Neurodegenerative Disease-related Compound Library

Anti-Obesity Compound Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Coagulation and Anti-coagulation Compound Library

Heterocyclic Compound Library

Off-patent Drug Library

Membrane Protein-targeted Compound Library

Membrane Receptor-targeted Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Lactylation Compound Library

Publications Citing Use of MedChemExpress (MCE) Ebastine

Alle Histamine Receptor Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Ebastine Related Classifications

HY-B0674 Related Classifications