Ebastine (LAS-W 090; RP64305)

Alias: LAS-W 090; RP-64305; LAS W 090; RP 64305; LAS-W-090; RP64305; Ebast; Ebatin; Ebatin Fast; Ebatrol; Atmos; Ebet; Ebastel FLAS; Kestine; KestineLIO
Cat No.:V1213 Purity: ≥98%
Ebastine (formerly LAS-W 090; RP-64305; LAS W090; RP64305; Ebast, Ebatin, Ebatrol, Atmos, Ebet, Kestine, KestineLIO) is a long-acting and selective H1-histamine receptor antagonist used for the treatment of allergic conditions.
Ebastine (LAS-W 090; RP64305) Chemical Structure CAS No.: 90729-43-4
Product category: Histamine Receptor
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
500mg
1g
2g
5g
10g
25g
Other Sizes

Other Forms of Ebastine (LAS-W 090; RP64305):

  • Ebastine-d5 (Ebastine d5)
Official Supplier of:
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Ebastine (formerly LAS-W 090; RP-64305; LAS W090; RP64305; Ebast, Ebatin, Ebatrol, Atmos, Ebet, Kestine, KestineLIO) is a long-acting and selective H1-histamine receptor antagonist used for the treatment of allergic conditions. Ebastine has low potential for causing drowsiness. It has a low likelihood of producing CNS side effects because it does not cross the blood–brain barrier (BBB).

Biological Activity I Assay Protocols (From Reference)
Targets
Histamine H1 receptor
ln Vitro

In vitro activity: Ebastine (10-500 ng/mL; 24-48 hours) treatment dramatically boosts HFDPC proliferation[2].
Ebastine (10-500 ng/mL; 24-48 hours) treatment results in dose-dependent increases in the expression levels of Cyclin D1, Cyclin E1, and Cyclin A. Additionally, there is an increase in the expression levels of Cdk4, Cdk2, and Cdc2. Extracellular signal-regulated kinase (phospho-AKT) and phospho-p44/42 are both expressed at higher levels when treated with ebastine[2].

ln Vivo
The plasma level of radioactivity in rats decreased biphasically with α-phase half-life (t1/2 α) of 1.6 h and β-phase half-life (t1/2 β) of 3.1 h following intravenous administration of [14C]Ebastine at a dose of 2 mg/kg[3].
The plasma level decreased monophasically with a t1/2 of 3.9 hours after the oral administration of 2 mg/kg of [14C]Ebastine, which caused it to reach its maximum (Cmax) of 102 ng eq/ml at 2 hours. A monophasic decrease is also noted at 20 mg/kg, with a t1/2 of 4.0 h and a Cmax of 1110 ng eq./ml at 4 h[3].
Cell Assay
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.
Animal Protocol
10 mg orally
N/A
References

[1]. Ebastine in allergic rhinitis and chronic idiopathic urticarial. Allergy. 2008 Dec;63 Suppl 89:1-20.

[2]. Extracellular Signal-Regulated Kinase Mediates Ebastine-Induced Human Follicle Dermal Papilla Cell Proliferation. Biomed Res Int. 2019 Feb 11;2019:6360503.

[3]. Absorption, distribution, metabolism and excretion of [14C]ebastine after a single administration in rats. Arzneimittelforschung. 1994 Apr;44(4):527-38.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C32H39NO2
Molecular Weight
469.66
Exact Mass
469.3
Elemental Analysis
C, 81.83; H, 8.37; N, 2.98; O, 6.81
CAS #
90729-43-4
Related CAS #
Ebastine-d5; 1216953-13-7
Appearance
Solid powder
SMILES
CC(C)(C)C1=CC=C(C=C1)C(=O)CCCN2CCC(CC2)OC(C3=CC=CC=C3)C4=CC=CC=C4
InChi Key
MJJALKDDGIKVBE-UHFFFAOYSA-N
InChi Code
InChI=1S/C32H39NO2/c1-32(2,3)28-18-16-25(17-19-28)30(34)15-10-22-33-23-20-29(21-24-33)35-31(26-11-6-4-7-12-26)27-13-8-5-9-14-27/h4-9,11-14,16-19,29,31H,10,15,20-24H2,1-3H3
Chemical Name
4-(4-benzhydryloxypiperidin-1-yl)-1-(4-tert-butylphenyl)butan-1-one
Synonyms
LAS-W 090; RP-64305; LAS W 090; RP 64305; LAS-W-090; RP64305; Ebast; Ebatin; Ebatin Fast; Ebatrol; Atmos; Ebet; Ebastel FLAS; Kestine; KestineLIO
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 4~93 mg/mL warmed (8.5~198.0 mM)
Water: <1 mg/mL
Ethanol: ~11 mg/mL (~23.4 mM)
Solubility (In Vivo)
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
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Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)


Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
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Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders


Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
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

*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.

Calculator

Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

  • Calculate the Mass of a compound required to prepare a solution of known volume and concentration
  • Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
  • Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume
An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
  • Enter 350.26 in the Molecular Weight (MW) box
  • Enter 10 in the Concentration box and choose the correct unit (mM)
  • Enter 5 in the Volume box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
  • Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
  • Enter 25 into the Concentration (End) box and select the correct unit (mM)
  • Enter 25 into the Volume (End) box and choose the correct unit (mL)
  • Click the “Calculate” button
  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
g/mol

Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
  • To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.
Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

  • Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
  • Click the “Calculate” button
  • The answer appears in the Volume (to add to vial) box
In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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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.

Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05815602 Recruiting Drug: Ebastine
Drug: Duspatalin
IBS - Irritable Bowel Syndrome
IBS
Guy Boeckxstaens March 30, 2023 Phase 3
NCT01908465 Completed Drug: Ebastine
Drug: Placebo
Irritable Bowel Syndrome (IBS) KU Leuven November 2013 Phase 4
NCT01144832 Completed Drug: ebastine
Drug: placebo capsule
Irritable Bowel Syndrome KU Leuven October 2009 Phase 4
Biological Data
  • Antihistamine effect of ebastine 10 mg. Allergy . 2008 Dec:63 Suppl 89:1-20.
  • Efficacy of ebastine in patients with seasonal allergic rhinitis. Comparisons of ebastine 10 and 20 mg once-daily (EBA 10; EBA 20) with loratadine 10 mg once-daily (LOR 10) and placebo (PL) for reduction in mean daily reflective total symptoms score during 4 weeks' treatment. Allergy . 2008 Dec:63 Suppl 89:1-20.
  • Efficacy of ebastine in patients with perennial allergic rhinitis. Comparison of ebastine 10 and 20 mg once-daily (EBA 10; EBA 20) with loratadine 10 mg once-daily (LOR 10) in the reduction of mean daily perennial index after 4 weeks' treatment. Allergy . 2008 Dec:63 Suppl 89:1-20.
  • Ebastine-induced HFDPC growth. HFDPC were plated in triplicate in 24-well plates for 24 h. Biomed Res Int . 2019 Feb 11:2019:6360503.
  • Ebastine enhanced the expression of cell cycle regulatory proteins in HFDPC. Biomed Res Int . 2019 Feb 11:2019:6360503.
  • Ebastine affected apoptosis-related proteins in HFDPC. Biomed Res Int . 2019 Feb 11:2019:6360503.
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