Azelastine

SKU: orb1310832

Description

Azelastine

Research Area

Immunology & Inflammation, Infectious Disease & Virology, Neuroscience, Pharmacology & Drug Discovery

Images & Validation

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Key Properties

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CAS Number	58581-89-8
MW	381.9
Purity	99.35% (May vary between batches)
Formula	C₂₂H₂₄ClN₃O
SMILES	CN1CCCC(CC1)n1nc(Cc2ccc(Cl)cc2)c2ccccc2c1=O
Target	Histamine Receptor\|\|\|SARS-CoV
Solubility	DMSO:3.82 mg/mL (10 mM)

Bioactivity

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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. 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. 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.

Storage & Handling

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Storage	-20°C
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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HistamineReceptor, Histamine Receptor, Inhibitor, H1 receptor, inhibit, Azelastina, Azelastine, Azelastinum, asthma, Astelin, antihistamine, allergic rhinitis, SARS-CoV, SARS coronavirus, SARSCoV

Quality Guarantee

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Compound Identifiers

PubChem CID

2267 ↗

Key Properties

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No computed properties available.

Protocol Information

Find More Protocols

CAS Number:	143228-84-6
MW:	381.9
Formula:	C₂₂H₂₄ClN₃O

CAS Number:	143228-85-7
MW:	381.9
Formula:	C₂₂H₂₄ClN₃O

Purity:	99.99% (May vary between batches)
CAS Number:	153408-28-7
MW:	418.36
Formula:	C₂₂H₂₅Cl₂N₃O

CAS Number:	153408-27-6
MW:	418.36
Formula:	C₂₂H₂₅Cl₂N₃O

CAS Number:	47491-38-3
MW:	367.87
Formula:	C₂₁H₂₂ClN₃O

Azelastine

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

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Desmethylazelastine [orb1982811]

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