Azelastine HCl - 10mM in DMSO , Histamine H1 receptor antagonist, CAS No.79307-93-0, Histamine H1 receptor antagonist

CAS: 79307-93-0 Cat. No.: A408950 Peso molecular: 418.36 Número EC: 620-469-0 PubChem CID: 54360

GRADE & PURITY 10mM in DMSO

Synonyms

4-​[(4-​chlorophenyl)​methyl]​-​2-​(hexahydro-​1-​methyl-​1H-​azepin-​4-​yl)​-​1(2H)​-​phthalazinone, hydrochloride (1:1)

Storage

Store at -80°C

Shipped In

Dry ice packs + Cold packs

Descripción general

Information

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

In vivo

Cell Data

cell lines：WTK1 lymphoblasts

Concentrations：

Incubation Time：

Powder Purity:≥99%

Specifications

Sinónimos

4-​[(4-​chlorophenyl)​methyl]​-​2-​(hexahydro-​1-​methyl-​1H-​azepin-​4-​yl)​-​1(2H)​-​phthalazinone, hydrochloride (1:1)

Especificaciones y pureza

10mM in DMSO

Mecanismos bioquímicos y fisiológicos

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

Condiciones de almacenamiento de almacenamiento

Store at -80°C

Enviado en

Dry ice packs + Cold packs

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Tipo de acción

ANTAGONIST

Mecanismo de acción

Histamine H1 receptor antagonist

Nombres e identificadores

• Isómeros SMILES: CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl.Cl
• RTECS: TH9203900
• PubChem CID: 54360
• Peso molecular: 418.36
• Reaxy-Rn: 4834474

Propiedades químicas y físicas

• Punto de fusión (°C): 226 °C