| Size | Price | Stock | Qty |
|---|---|---|---|
| 500mg |
|
||
| 1g |
|
||
| 2g |
|
||
| 5g |
|
||
| 10g |
|
||
| 25g |
|
||
| Other Sizes |
|
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
|
||
|---|---|---|---|
| ln Vitro |
|
||
| ln Vivo |
|
||
| 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 |
|
||
| ADME/Pharmacokinetics |
Metabolism / Metabolites
Ebastine has known human metabolites that include 4-(4-tert-butylphenyl)-4-oxobutanal and Deslakylebastine. |
||
| Toxicity/Toxicokinetics |
Effects During Pregnancy and Lactation
◉ Summary of Use during Lactation Ebastine is a nonsedating antihistamine that is not available in the United States, but is available in other countries. Preliminary evidence indicates that the amounts in milk are unlikely to affect a breastfed infant. ◉ Effects in Breastfed Infants A woman with chronic urticaria was taking ebastine 10 mg daily during pregnancy and postpartum. Her infant was exclusively breastfed until the age of 6 months. He showed normal development at 1 and 3 months of age. ◉ Effects on Lactation and Breastmilk Antihistamines in relatively high doses given by injection can decrease basal serum prolactin in nonlactating women and in early postpartum women. However, suckling-induced prolactin secretion is not affected by antihistamine pretreatment of postpartum mothers. Whether lower oral doses of antihistamines or ebastine have the same effect on serum prolactin or whether the effects on prolactin have any consequences on breastfeeding success have not been studied. The prolactin level in a mother with established lactation may not affect her ability to breastfeed. |
||
| References |
|
||
| Additional Infomation |
Ebastine is an organic molecular entity.
Ebastine is under investigation for the treatment of Irritable Bowel Syndrome (IBS). Ebastine has been investigated for the treatment of Urticaria. |
| Molecular Formula |
C32H39NO2
|
|
|---|---|---|
| Molecular Weight |
469.66
|
|
| Exact Mass |
469.298
|
|
| 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
|
|
| PubChem CID |
3191
|
|
| Appearance |
White to off-white solid powder
|
|
| Density |
1.1±0.1 g/cm3
|
|
| Boiling Point |
596.3±50.0 °C at 760 mmHg
|
|
| Melting Point |
80-82°C
|
|
| Flash Point |
314.5±30.1 °C
|
|
| Vapour Pressure |
0.0±1.7 mmHg at 25°C
|
|
| Index of Refraction |
1.590
|
|
| LogP |
7.79
|
|
| Hydrogen Bond Donor Count |
0
|
|
| Hydrogen Bond Acceptor Count |
3
|
|
| Rotatable Bond Count |
10
|
|
| Heavy Atom Count |
35
|
|
| Complexity |
594
|
|
| Defined Atom Stereocenter Count |
0
|
|
| SMILES |
O=C(CCCN1CCC(OC(C2C=CC=CC=2)C2C=CC=CC=2)CC1)C1C=CC(C(C)(C)C)=CC=1
|
|
| 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 |
|
|
| 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 (In Vitro) |
|
|||
|---|---|---|---|---|
| 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 |
|
|
|
|
|
|
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
COA
