盐酸氮卓斯汀 /Azelastine HCl
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货号：A341055
同义名：
氮卓斯汀盐酸盐
/ Azelastine (hydrochloride);Azelastine hydrochloride
Azelastine HCl is a selective antagonist of histamine receptor used in the treatment of rhinitis.
Azelastine HCl 化学结构
Azelastine HCl 3D分子结构
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Azelastine HCl 纯度/质量文件 产品仅供科研
货号：A341055
标准纯度：
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产品说明书
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Azelastine HCl 质控信息
Hydroxyzine 2HCl
99+%
Cyclizine
✔
97%
Loratadine
+
98%
Desloratadine
++
Histamine H1 receptor, IC50: 51 nM
98%
Doxylamine succinate
✔
99%
Ebastine
✔
98%
Tripelennamine HCl
+
98%
Meclizine dihydrochloride
✔
98%
Chlorpheniramine maleate
+++
Histamine H1 receptor, IC50: 12 nM
99%
Diphenhydramine HCl
✔
99%
Alcaftadine
++++
++
99%+
Fexofenadine HCl
++
Histamine H1 receptor, IC50: 246 nM
99%+
Bilastine
+++
H1 receptor, Ki: 44.15 nM
98%
Pemirolast potassium
✔
98%
Bepotastine besilate
+
Histamine H1 receptor, pIC50: 5.7
98%
Mizolastine
+++
Histamine H1 receptor, IC50: 47 nM
98%
Brompheniramine maleate
✔
98%
Carbinoxamine maleate salt
✔
99+%
Clemastine fumarate
++++
Histamine H1 receptor, IC50: 3 nM
98%
Ketotifen fumarate salt
✔
95%
Rupatadine Fumarate
++
Histamine H1 receptor, Ki: 102 nM
PAFR
98%
Famotidine
✔
97%
Roxatidine Acetate HCl
+
Histamine H2 receptor, IC50: 3.2 μM
98%
Lafutidine
✔
99%
Cimetidine
✔
98%
Nizatidine
++++
Histamine H2 receptor, IC50: 0.9 nM
AChE
98%
Ranitidine
✔
98%
Betahistine
+
Histamine H3 receptor, IC50: 1.9 μM
98%
Ciproxifan maleate
+++
Histamine H3 receptor, IC50: 9.2 nM
99%+
S 38093
++
human H3 receptor, Ki: 1.2 μM
rat H3 receptor, Ki: 1.44 μM
98%
JNJ-7777120
++++
Histamine H4 receptor, Ki: 4.5 nM
98%
Azelastine HCl
✔
98%
Epinastine HCl
✔
98%
Levodropropizine
✔
97%
Cyproheptadine hydrochloride
✔
98%
Hesperetin
✔
97%
Olopatadine HCl
✔
98%
Mianserin hydrochloride
✔
99+%
Buclizine 2HCl
✔
97%
Latrepirdine 2HCl
✔
GluR
98%
Cetirizine 2HCl
✔
98%
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
Azelastine HCl 生物活性
靶点
描述
Azelastine Hydrochloride is an effective, rapid-acting, and well-tolerated second-generation antihistamine that improves nasal symptoms associated with SAR (seasonal allergic rhinitis) and VMR (vasomotor rhinitis). Azelastine hydrochloride (azelastine) nasal spray is a histamine receptor-1 (H1) antagonist often used in treating allergic rhinitis to relieve its symptoms. Addition of azelastine at doses of 1μM or above elicited a significant dilation response to 1μM methoxamine-induced mucosal contraction. Azelastine could inhibit electrical field stimulation-induced spike mucosal contraction. Moreover, increase in concentration of azelastine had minimal effect on basal tension of nasal mucosa[3] [4]
Azelastine HCl 参考文献
[1] Hide I, Toriu N, et al. Suppression of TNF-alpha secretion by azelastine in a rat mast (RBL-2H3) cell line: evidence for differential regulation of TNF-alpha release, transcription, and degranulation. J Immunol. 1997 Sep 15;159(6):2932-40.
[2] Yoneda K, Yamamoto T, et al. Suppression by azelastine hydrochloride of NF-kappa B activation involved in generation of cytokines and nitric oxide. Jpn J Pharmacol. 1997 Feb;73(2):145-53.
[3] Cheng LH, Lee JC, Wu PC, Lin YY, Chu YH, Wang HW. Azelastine nasal spray inhibiting sympathetic function on human nasal mucosa in patients with allergy rhinitis. Rhinology. 2019 Aug 1;57(4):268-272
[4] Karpishchenko SA, Kolesnikova OM. Éffektivnost' kombinatsii azelastina gidrokhlorida i mometazona furoata dlia intranazal'nogo primeneniia u bol'nykh sezonnym allergicheskim rinitom [The effectiveness of the combination of azelastine hydrochloride and mometasone furoate for the intranasal application in the patients presenting with seasonal allergic rhinitis]. Vestn Otorinolaringol. 2017;82(5):44-47. Russian
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Azelastine HCl 实验方案
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摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
2.39mL
0.48mL
0.24mL
11.95mL
2.39mL
1.20mL
23.90mL
4.78mL
2.39mL
Azelastine HCl 技术信息
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