Azelastine
Based on 3 publication(s) in Google Scholar
Azelastine, an antihistamine, is a potent and selective histamine 1 (H1) antagonist. Azelastine can be used for the research of allergic rhinitis, asthma, diabetic hyperlipidemic and SARS-CoV-2.
For research use only. We do not sell to patients.
- Purity: 99.92%
- CAS No.: 58581-89-8
- Formula: C22H24ClN3O
- Molecular Weight:381.90
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Azelastine
MoreAll Histamine Receptor Isoforms
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Biological Activity
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H1 Receptor |
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Cell Line
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Type | Value | Description | References |
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| LLC-PK1 | IC50 |
16 μM
Compound: Azelastine
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TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Daunorubicin transepithelial transport (basal to apical) (Daunorubicin: 0.035 uM) in MDR1-expressing LLC-PK1 cells
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[PMID: 11231118] |
| LLC-PK1 | IC50 |
30 μM
Compound: Azelastine
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TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.025 uM) in MDR1-expressing LLC-PK1 cells
TP_TRANSPORTER: inhibition of Digoxin transepithelial transport (basal to apical) (Digoxin: 0.025 uM) in MDR1-expressing LLC-PK1 cells
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[PMID: 11231118] |
| Ventricular myocyte | IC50 |
20.2 μM
Compound: Azelastine
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Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
Inhibition of L-type calcium channel measured using whole-cell patch clamp in guinea pig ventricular myocytes
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[PMID: 22761000] |
Azelastine can significantly inhibit HNEpC proliferation, and therefore, be helpful in against airway remodeling[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human nasal epithelial cells (HNEpC)
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Concentration:100 μM, 400 μM
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Incubation Time:21 days
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Result:Inhibited HNEpC growth.
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Cell Line:Human nasal epithelial cells (HNEpC)
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Concentration:100 μM
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Incubation Time:7 days
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Result:Significantly up-regulated the H1R, M1R and M3R levels.
Azelastine (4 mg/kg; p.o.; daily; for 8 weeks) improves the lipid profile (LDL-c decrease and HDL-c increase) in diabetic hyperlipidemic rats model[2].
Azelastine (4 mg/kg; p.o.; daily; for 8 weeks) attenuates calcium deposition and aortic calcification in diabetic hyperlipidemic rats model[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male albino Wistar rats (150-170 g), diabetic hyperlipidemic rats model[2]
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Dosage:4 mg/kg
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Administration:Oral administration, daily, for 8 weeks
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Result:Ameliorated aortic calcification and increased apolipoprotein A expression along with a decline in apolipoprotein B.
Chemical Information
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CAS No. 58581-89-8
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Appearance Solid
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Molecular Weight 381.90
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Formula C22H24ClN3O
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Color White to off-white
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SMILES
O=C1N(C2CCN(C)CCC2)N=C(CC3=CC=C(Cl)C=C3)C4=C1C=CC=C4
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Publications (3)
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Journal Impact Factor
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Most Recent
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Phytomedicine
Alpha-linolenic acid improves nasal mucosa epithelial barrier function in allergic rhinitis by arresting CD4+ T cell differentiation via IL-4Rα-JAK2-STAT3 pathway. [Abstract]2023 Jul 25:116:154825. PMID: 37178572 -
Pharm Res
Investigation of the Binding Characteristics of Agonists and Various Antagonists Targeting Histamine 1 Receptor. [Abstract]2025 Aug;42(8):1315-1329. PMID: 40760405 -
Solvent & Solubility
DMSO : 100 mg/mL (261.85 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)
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 5 mg/mL (13.09 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 5 mg/mL (13.09 mM); Clear solution
This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (280 KB)
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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)
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Handling Instructions (2659 KB)
References
[1]. Craig La Force. Review of the pharmacology, clinical efficacy, and safety of azelastine hydrochloridel. Expert Rev Clin Immunol. 2005 Jul;1(2):191-201. [Content Brief]
[2]. Mohamed M Elseweidy, et al. Azelastine a potent antihistamine agent, as hypolipidemic and modulator for aortic calcification in diabetic hyperlipidemic rats model. Arch Physiol Biochem. 2020 Jul 2;1-8. [Content Brief]
[3]. Carlos D. Zappia, et al. Azelastine potentiates antiasthmatic dexamethasone effect on a murine asthma model. Pharmacol Res Perspect. 2019 Dec; 7(6): e00531. [Content Brief]
[4]. Li Yang, et al. Identification of SARS-CoV-2 entry inhibitors among already approved drugs. Acta Pharmacol Sin. 2020 Oct 28 : 1-7. [Content Brief]
[5]. Shao-Cheng Liu, et al. Effect of budesonide and azelastine on histamine signaling regulation in human nasal epithelial cells. Eur Arch Otorhinolaryngol. 2017 Feb;274(2):845-853. [Content Brief]
Complete Stock Solution Preparation Table
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 2.6185 mL | 13.0924 mL | 26.1849 mL | 65.4622 mL |
| 5 mM | 0.5237 mL | 2.6185 mL | 5.2370 mL | 13.0924 mL | |
| 10 mM | 0.2618 mL | 1.3092 mL | 2.6185 mL | 6.5462 mL | |
| 15 mM | 0.1746 mL | 0.8728 mL | 1.7457 mL | 4.3641 mL | |
| 20 mM | 0.1309 mL | 0.6546 mL | 1.3092 mL | 3.2731 mL | |
| 25 mM | 0.1047 mL | 0.5237 mL | 1.0474 mL | 2.6185 mL | |
| 30 mM | 0.0873 mL | 0.4364 mL | 0.8728 mL | 2.1821 mL | |
| 40 mM | 0.0655 mL | 0.3273 mL | 0.6546 mL | 1.6366 mL | |
| 50 mM | 0.0524 mL | 0.2618 mL | 0.5237 mL | 1.3092 mL | |
| 60 mM | 0.0436 mL | 0.2182 mL | 0.4364 mL | 1.0910 mL | |
| 80 mM | 0.0327 mL | 0.1637 mL | 0.3273 mL | 0.8183 mL | |
| 100 mM | 0.0262 mL | 0.1309 mL | 0.2618 mL | 0.6546 mL |
Azelastine Related Classifications
HY-B0462A Related Classifications
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