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Azelastine

Catalog No. T0211 CAS 58581-89-8

Synonyms: Azelastina, Astelin, Azelastinum

Azelastine (Azelastinum) is a phthalazine derivative, and is an histamine antagonist and mast cell stabilizer.

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Azelastine, CAS 58581-89-8

Pack Size	Availability	Price/USD	Quantity
100 mg	In stock	$ 50.00
1 mL * 10 mM (in DMSO)	In stock	$ 45.00

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Purity: 99.35%

Biological Description

Chemical Properties

Storage & Solubility Information

Description

Azelastine (Azelastinum) is a phthalazine derivative, and is an histamine antagonist and mast cell stabilizer.

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]

Synonyms	Azelastina, Astelin, Azelastinum
Molecular Weight	381.9
Formula	C22H24ClN3O
CAS No.	58581-89-8

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 3.82 mg/mL (10 mM)

References and Literature

1. Hide I, et al. J Immunol,1997, 159(6), 2932-2940. 2. Yoneda K, et al. Jpn J Pharmacol,1997, 73(2), 145-153. 3. Kempuraj D, et al. Int Arch Allergy Immunol,2003, 132(3), 231-239.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Drug Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library GPCR Compound Library Inhibitor Library Anti-Neurodegenerative Disease Compound Library Bioactive Compound Library Anti-Viral Compound Library Neuronal Signaling Compound Library Orally Active Compound Library

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SARS-CoV-2-IN-59 GRL0617 ZINC475239213 D1N8 SARS-CoV-2-IN-63 MTase-IN-1 SARS-CoV-2-IN-44 SARS-CoV-2 nsp14-IN-4

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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc.

Keywords

Azelastine 58581-89-8 GPCR/G Protein Immunology/Inflammation Microbiology/Virology Neuroscience SARS-CoV Histamine Receptor antihistamine inhibit Inhibitor Azelastina asthma allergic rhinitis Astelin Azelastinum SARS coronavirus inhibitor

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