Azelastine HCl

Catalog No.S2552

Azelastine HCl Chemical Structure

Molecular Weight(MW): 418.36

Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.

Size Price Stock Quantity  
In DMSO USD 70 In stock
USD 50 In stock
USD 70 In stock
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Biological Activity

Description Azelastine HCl is a potent, second-generation, selective, histamine receptor antagonist, used in the treatment of rhinitis.
Targets
Histamine receptor [1]
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
Synonyms N/A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03004131 Recruiting Seasonal Allergic Rhinitis MEDA Pharma GmbH & Co. KG January 7, 2017 Phase 4
NCT02953106 Not yet recruiting Asthma, Allergic|Rhinitis,Allergic|Allergy University of Dundee December 2016 Phase 4
NCT02557269 Active, not recruiting Seasonal Allergic Rhinitis Association Asthma, Bulgaria|Nasaleze May 2015 Phase 4
NCT02402465 Recruiting Allergic Rhinitis University of Chicago February 2015 Phase 4
NCT02238353 Recruiting 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

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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.

Handling Instructions

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID