Azelastine HCl
Catalog No.S2552
Molecular Weight(MW): 418.36
Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
Purity & Quality Control
Choose Selective Histamine Receptor Inhibitors
Biological Activity
| Description | Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis. | |
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| Targets |
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| In vitro |
Azelastine inhibits Ag- and ionomycin-induced TNF-alpha release with IC50 values of 25.7 mM and 1.66 mM, respectively, in a rat mast RBL-2H3 cell line. Azelastine also inhibits TNF-alpha mRNA expression, TNF-alpha protein synthesis and release, and, possibly related to these effects, Ca2+ influx, in Ag-stimulated cells. Azelastine inhibits TNF-alpha release to a greater extent than mRNA expression/protein synthesis and Ca2+ influx in ionomycin-stimulated cells, suggesting that Azelastine inhibits the release process more potently than transcription or production of TNF-alpha by interfering with a signal other than Ca2+. Azelastine added 1 hour after ionomycin stimulation also immediately blocks subsequent release of TNF-alpha, which has been produced in the cells, without affecting Ca2+ influx. Azelastine inhibits ionomycin-induced, but not Ag-induced, protein kinase C translocation to the membranes. [1] Azelastine hydrochloride (Azeptin) dose-dependently suppresses both DNA and protein synthesis in human gingival fibroblasts (HF) and also suppresses blastogenesis of human peripheral blood lymphocytes (PBL). Azelastine hydrochloride (Azeptin) suppresses both inducible nitric oxide synthase-mRNA level and NO generation in mouse peritoneal macrophages. [2] Azelastine inhibits secretion of IL-6, TNF-alpha and IL-8 as well as NF-kappaB activation and intracellular calcium ion levels in normal human mast cells. [3] |
Protocol
Solubility (25°C)
| In vitro | Ethanol | 42 mg/mL (100.39 mM) |
|---|---|---|
| Water | 35 mg/mL (83.66 mM) | |
| DMSO | 28 mg/mL (66.92 mM) |
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
Chemical Information
| Molecular Weight | 418.36 |
|---|---|
| Formula | C22H24ClN3O.HCl |
| CAS No. | 79307-93-0 |
| Storage | powder |
| in solvent | |
| Synonyms | N/A |
Bio Calculators
Molarity Calculator
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Dilution Calculator
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Molarity Calculator
Clinical Trial Information
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT02953106 | Recruiting | Asthma Allergic|RhinitisAllergic|Allergy | University of Dundee | December 2016 | Phase 4 |
| NCT02238353 | Unknown status | Allergic Rhinitis|House Dust Mite Allergy | Universitaire Ziekenhuizen Leuven | October 2014 | Phase 4 |
| NCT02249663 | Unknown status | Seasonal Allergic Rhinitis | Teva Pharmaceuticals USA | August 2014 | Phase 3 |
| NCT02279563 | Unknown status | Seasonal Allergic Rhinitis | Apotex Inc. | December 2013 | Phase 2 |
| NCT01470053 | Completed | Perennial Allergic Rhinitis | Hanlim Pharm. Co. Ltd. | March 2011 | Phase 3 |
| NCT01190852 | Completed | Allergic Rhinitis | MEDA Pharma GmbH & Co. KG|ClinResearch GmbH|Prolytic GmbH | August 2010 | Phase 1 |
Tech Support
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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