Name: Ebastine
Brand: Selleck Chemicals
SKU: S4262
Availability: InStock
Rating: 5 (4 reviews)

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Quality Control

Batch: Purity: 99.86%

99.86

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Histamine Receptor Inhibitors	GSK2879552 Dihydrochloride JNJ-7777120 Mianserin HCl Ciproxifan Maleate Dimethindene maleate Rupatadine Levodropropizine Chloropyramine hydrochloride Lafutidine Betahistine mesylate

Solubility

In vitro
Batch:

DMSO : 93 mg/mL (198.01 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 93 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

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%

Calculation results:

Working concentration: mg/ml;

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.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	469.66	Formula	C₃₂H₃₉NO₂	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	90729-43-4	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	LAS-W 090,RP64305			Smiles	CC(C)(C)C1=CC=C(C=C1)C(=O)CCCN2CCC(CC2)OC(C3=CC=CC=C3)C4=CC=CC=C4

Mechanism of Action

Targets/IC₅₀/Ki	Histamine H1 receptor
In vitro	Ebastine at concentrations approximating those found in plasma under certain conditions suppresses in a voltage-independent manner the I(Kr) (Kd = 0.14 μM, maximum block 74%) more effectively than the slowly delayed rectifier K+ current (I(Ks)) (Kd = 0.8 μM, maximum block 60%) in guinea pig ventricular myocytes. This compound also suppresses IKr in HERG-expressing X. laevis oocytes with the K d value of 0.3 μM and a maximal block of 46% at 3 μM. It produces negligible effect on rat transient K+ current at concentrations of <100 nM. This chemical is shown to block the release of anti-IgE-induced prostaglandin D2 (PGD2) and leukotriene C4/D4 from human nasal polyp cells (IC30 values of 2.57 and 9.6 μM, respectively) and to inhibit the release of cytokines. It is a novel histamine H1 receptor antagonist that combines potency with a rapid onset (fast absorption) and long duration (slow elimination) of action, at least partially mediated via the formation of an acid metabolite (carebastine) that is even more potent as an antihistamine. This agent has negligible activity against acetylcholine (no atropine-like adverse effects on secretions and visual accommodation) and only poorly penetrates the blood-brain barrier (no sedative adverse effects). It is without effects on the central nervous and cardiovascular systems, even after oral administration of high doses, and does not interact pharmacologically with a wide range of other drugs covering most areas of potential coadministration. This compound shows clear selectivity for histamine H1 as opposed to H2 receptors, has moderate activity against other potential mediators of allergic phenomena such as leukotriene C4 and platelet-activating factor, and is clearly effective against anaphylactic reactions resulting from exposure of suitably sensitised tissues or animals to antigen.
References	[1] https://pubmed.ncbi.nlm.nih.gov/9103502/ [2] https://pubmed.ncbi.nlm.nih.gov/8983912/ [3] https://pubmed.ncbi.nlm.nih.gov/8828021/

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Ebastine Histamine Receptor antagonist

Chemical Structure

Molecular Weight: 469.66