| Size | Price | Stock | Qty |
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| 500mg |
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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 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).
| Targets |
Histamine H1 receptor
Histamine H1 receptor (H1R) (human H1R, Ki=0.9 nM; rat H1R, Ki=1.2 nM) [1] Extracellular signal-regulated kinase (ERK) (mediates cell proliferation) [2] |
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| 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]. Human peripheral blood basophils were stimulated with anti-IgE (1 μg/mL). Ebastine (LAS-W 090; RP64305) (1 nM-10 μM) dose-dependently inhibited histamine release, with maximum inhibition of 72% at 10 μM, confirming H1R antagonistic activity [1] - Human follicle dermal papilla cells (HFDPCs) were treated with Ebastine (LAS-W 090; RP64305) (0.1 μM-50 μM) for 24-48 hours. The drug promoted cell proliferation in a concentration-dependent manner, with 48-hour cell viability increased by 35% at 10 μM and 52% at 50 μM (CCK-8 assay). Western blot showed it upregulated phosphorylation of ERK1/2 (p-ERK1/2) by 2.3-fold at 10 μM, which was blocked by ERK inhibitor PD98059 [2] - Isolated guinea pig tracheal smooth muscle strips pre-contracted with histamine (1 μM) were treated with Ebastine (LAS-W 090; RP64305) (0.1 μM-10 μM). It induced concentration-dependent relaxation, with EC50=1.5 μM, via competitive H1R blockade [1] |
| 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]. Passive cutaneous anaphylaxis (PCA) model in rats: Oral administration of Ebastine (LAS-W 090; RP64305) (0.3 mg/kg, 1 mg/kg, 3 mg/kg) 1 hour before antigen challenge dose-dependently inhibited skin wheal formation, with maximum inhibition of 82% at 3 mg/kg [1] - Allergic rhinitis model in guinea pigs: Intranasal administration of ovalbumin induced nasal symptoms (sneezing, rhinorrhea). Oral Ebastine (LAS-W 090; RP64305) (1 mg/kg/day) for 7 days reduced sneezing frequency by 65% and nasal secretion by 58%, associated with decreased nasal mucosal histamine levels [1] - Chronic idiopathic urticaria (CIU) clinical trial: Adult patients treated with oral Ebastine (LAS-W 090; RP64305) (10 mg/day) for 4 weeks showed 70% reduction in wheal number and 68% reduction in pruritus severity compared to placebo. Symptom relief was sustained for 24 hours post-administration [1] |
| Enzyme Assay |
H1R binding assay: Prepare membrane fractions from human H1R-expressing HEK293 cells or rat brain tissue. Incubate membranes with [3H]-pyrilamine (0.5 nM) and various concentrations of Ebastine (LAS-W 090; RP64305) (0.01 nM-100 nM) at 25°C for 60 minutes. Separate bound and free ligand by vacuum filtration through glass fiber filters. Measure radioactivity with a liquid scintillation counter and calculate Ki values using the Cheng-Prusoff equation [1]
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| 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. Basophil histamine release assay: Isolate human peripheral blood basophils via density gradient centrifugation. Resuspend cells in buffer and pre-treat with Ebastine (LAS-W 090; RP64305) (1 nM-10 μM) for 30 minutes. Stimulate with anti-IgE (1 μg/mL) for 60 minutes at 37°C. Centrifuge to collect supernatant and measure histamine concentration via fluorometric assay [1] - HFDPC proliferation and ERK activation assay: Seed HFDPCs in 96-well plates (for viability) or 6-well plates (for Western blot) at 5×103 cells/well and 2×105 cells/well respectively. Incubate for 24 hours, then treat with Ebastine (LAS-W 090; RP64305) (0.1 μM-50 μM) for 24-48 hours. For viability, add CCK-8 reagent and measure absorbance at 450 nm. For ERK activation, extract protein, perform Western blot with anti-p-ERK1/2 and anti-total ERK1/2 antibodies, and quantify band intensity [2] - Tracheal smooth muscle relaxation assay: Isolate guinea pig tracheal strips, mount in organ baths with oxygenated Krebs-Ringer solution (37°C, 95% O2/5% CO2), and equilibrate for 60 minutes. Pre-contract with histamine (1 μM), then add Ebastine (LAS-W 090; RP64305) (0.1 μM-10 μM) cumulatively and record tension changes [1] |
| Animal Protocol |
10 mg orally
PCA rat model: Male Wistar rats (150-200 g) were intradermally injected with anti-ovalbumin IgE (0.1 mL) on the back. After 48 hours, Ebastine (LAS-W 090; RP64305) was dissolved in 0.5% carboxymethylcellulose sodium and administered via oral gavage (0.3 mg/kg, 1 mg/kg, 3 mg/kg). One hour later, intravenous injection of ovalbumin (1 mg/kg) + Evans blue (5 mg/kg) was given. Thirty minutes later, rats were euthanized, and skin wheal area was measured [1] - Allergic rhinitis guinea pig model: Male Hartley guinea pigs (300-350 g) were sensitized with ovalbumin (100 μg) + aluminum hydroxide (2 mg) via intraperitoneal injection on days 0 and 7. From day 14, intranasal ovalbumin (1% solution) was administered once daily for 7 days to induce rhinitis. Ebastine (LAS-W 090; RP64305) (1 mg/kg) was given via oral gavage once daily 1 hour before ovalbumin challenge. Record sneezing and nasal secretion for 10 minutes post-challenge [1] - Pharmacokinetic rat experiment: Male Sprague-Dawley rats (200-250 g) were fasted for 12 hours. Ebastine (LAS-W 090; RP64305) labeled with [14C] was administered via oral gavage (10 mg/kg) or intravenous injection (2 mg/kg). Blood, tissues (liver, kidney, brain, etc.), urine, and feces were collected at predetermined time points. Radioactivity was measured to determine drug concentration and distribution/excretion profiles [3] |
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Ebastine's known metabolites include 4-(4-tert-butylphenyl)-4-oxobutyraldehyde and dealkylebastine. Absorption: Oral bioavailability in rats is 60-70%; peak plasma concentration (Cmax) is reached 2-3 hours after oral administration. In humans, the oral bioavailability is 90%, and the Cmax at a 10 mg dose is 13 ng/mL [1,3] -Distribution: The volume of distribution (Vd) in rats is 15-18 L/kg; it is widely distributed in various tissues, with a brain/plasma concentration ratio <0.1 (very low blood-brain barrier penetration) [3] -Metabolism: It is mainly metabolized in the liver by cytochrome P450 (CYP) 3A4 to produce carbastine (active metabolite), which accounts for more than 90% of the plasma active compound [1,3] -Excretion: 70% of the dose is excreted in feces (50% as metabolites, 20% as the original drug), and 25% is excreted in urine (mainly as metabolites). The elimination half-life (t1/2) in rats is 10-12 hours, and in humans it is 15-19 hours (carbastine t1/2 = 20-24 hours) [1,3] |
| Toxicity/Toxicokinetics |
Medication Use During Pregnancy and Lactation ◉ Overview of Medication Use During Lactation
Ebastine is a non-sedating antihistamine not marketed in the United States but available in other countries. Preliminary evidence suggests that the amount of the drug in breast milk is unlikely to affect breastfed infants. ◉ Effects on Breastfed Infants A woman with chronic urticaria took 10 mg of ebastine daily during pregnancy and postpartum. Her infant was exclusively breastfed until 6 months of age. The infant developed normally at 1 month and 3 months of age. ◉ Effects on Lactation and Breast Milk Higher doses of antihistamines can lower basal serum prolactin levels in non-lactating women and early postpartum women. However, pre-administration of antihistamines by postpartum mothers does not affect lactation-induced prolactin secretion. Whether low-dose oral antihistamines or ebastine have the same effect on serum prolactin, and whether this effect on prolactin has any impact on breastfeeding success, has not been studied. Prolactin levels in established lactating mothers may not affect their ability to breastfeed. Plasma protein binding rate: The plasma protein binding rate of ebastine (LAS-W 090; RP64305) and its metabolite carbastine in human plasma is 95-97%[1] - Acute toxicity: The LD50 (oral) in rats and mice is >2000 mg/kg; no deaths or serious clinical symptoms (ataxia, convulsions) have been reported[1] - Chronic toxicity: No significant hepatotoxicity, hematological abnormalities or organ weight changes were observed in rats after oral administration of ebastine (LAS-W 090; RP64305) (100 mg/kg/day) for 6 months[1] - Clinical side effects: Mild headache (4-6% of patients), fatigue (2-3%) and dry mouth (1-2%) have been reported. No sedation or cognitive impairment was observed at therapeutic doses [1] - Drug interactions: Co-administration with CYP3A4 inhibitors (e.g., ketoconazole) can increase plasma carbastine concentration by 30-40%; no significant interactions with other CYP isoenzyme substrates [1] |
| References |
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| Additional Infomation |
Ebastine is an organic molecular entity. Ebastine is being investigated for the treatment of irritable bowel syndrome (IBS). Ebastine has been investigated for the treatment of urticaria. Ebastine (LAS-W 090; RP64305) is a second-generation non-sedating histamine H1 receptor antagonist, whose main active metabolite is carbastine [1,3]. Its main mechanism of action is competitive binding to H1 receptors, blocking histamine-mediated allergic reactions (increased vascular permeability, smooth muscle contraction, and cytokine release) [1]. It promotes the proliferation of human hair follicle dermal papilla cells by activating the ERK signaling pathway, suggesting its potential application value in promoting hair growth [2]. Indications include allergic rhinitis (relief of sneezing, runny nose, and nasal itching) and chronic idiopathic urticaria (relief of wheals and itching) [1]. Its low blood-brain barrier penetration and high selectivity for H1 receptors are key factors in its therapeutic effect. It does not have a sedative effect, which distinguishes it from first-generation antihistamines [1,3]
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| Molecular Formula |
C32H39NO2
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| Molecular Weight |
469.66
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| Exact Mass |
469.298
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| Elemental Analysis |
C, 81.83; H, 8.37; N, 2.98; O, 6.81
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| CAS # |
90729-43-4
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| Related CAS # |
Ebastine-d5; 1216953-13-7
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| PubChem CID |
3191
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| Appearance |
White to off-white solid powder
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| Density |
1.1±0.1 g/cm3
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| Boiling Point |
596.3±50.0 °C at 760 mmHg
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| Melting Point |
80-82°C
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| Flash Point |
314.5±30.1 °C
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| Vapour Pressure |
0.0±1.7 mmHg at 25°C
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| Index of Refraction |
1.590
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| LogP |
7.79
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
35
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| Complexity |
594
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| Defined Atom Stereocenter Count |
0
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| SMILES |
O=C(CCCN1CCC(OC(C2C=CC=CC=2)C2C=CC=CC=2)CC1)C1C=CC(C(C)(C)C)=CC=1
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| InChi Key |
MJJALKDDGIKVBE-UHFFFAOYSA-N
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| 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
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| Chemical Name |
4-(4-benzhydryloxypiperidin-1-yl)-1-(4-tert-butylphenyl)butan-1-one
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| 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
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *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 : PEG300 ：Tween 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). View More
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)] 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). View More
Oral Formulation 3: Dissolved in PEG400 (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.
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.
| 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 |
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