计算溶液所需的质量、体积或浓度。
概述
Azelastine HCl是有效的，第二代选择性组胺拮抗剂。An H1-receptor antagonist with antiallergic effects and disrupts TNF alpha activity.
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%
规格
规格或纯度
10mM in DMSO
英文名称
Azelastine HCl
生化机理
盐酸氮卓斯汀是一种强效的第二代选择性组胺受体拮抗剂，用于治疗鼻炎。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
拮抗剂
作用机制
组胺 H1 受体拮抗剂
名称和识别符
EC号
620-469-0
分子类型
小分子
Isomeric SMILES
CN1CCCC(CC1)N2C(=O)C3=CC=CC=C3C(=N2)CC4=CC=C(C=C4)Cl.Cl
PubChem CID
分子量
418.36
Reaxy-Rn
4834474
高级数据
化学和物理性质
熔点
226 °C
安全和危险性（GHS）
象形图
信号词
警告
危险声明
H227: 可燃液体
预防措施声明
P210: 远离热源，热表面，火花，明火和其他点火源。 - 禁止抽烟。
P280: 戴防护手套/穿防护服/戴防护眼罩/戴防护面具。
P370+P378: 火灾时：使用干砂、干粉或抗醇泡沫灭火。
P403+P235: 存放在通风良好的地方。保持低温。
P501: 将内容物/容器送到批准的废物处理厂处理
RTECS
TH9203900
Merck Index
906
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技术文档和文章
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