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Azelastine
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Azelastine图片
CAS NO:58581-89-8
包装与价格:
包装价格(元)
50 mg电议
100 mg电议

产品名称
Azelastinum
Azelastina
Astelin
氮卓斯汀
产品介绍
Azelastine 是一种选择性组胺 1 拮抗剂,可研究过敏性鼻炎、哮喘、糖尿病高脂血症和 SARS-CoV-2 。

产品描述

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

体外活性

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]

Cas No.

58581-89-8

分子式

C22H24ClN3O

分子量

381.9

别名

Azelastinum;Azelastina;Astelin;氮卓斯汀

储存和溶解度

DMSO:Soluble
Powder: -20°C for 3 years
In solvent: -80°C for 2 years