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盐酸氮卓斯汀 /Azelastine HCl {[allProObj[0].p_purity_real_show]}

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 CAS号:79307-93-0
Azelastine HCl 化学结构
CAS号:79307-93-0
Azelastine HCl 3D分子结构
CAS号:79307-93-0
Azelastine HCl 化学结构 CAS号:79307-93-0
Azelastine HCl 3D分子结构 CAS号:79307-93-0
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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: {[allProObj[0].p_purity_real_show]}
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产品名称 H1 receptor H2 receptor H3 receptor H4 receptor Histamine receptor 其他靶点 纯度
Hydroxyzine 2HCl 99+%
Cyclizine 97%
Loratadine +

B(0)AT2, IC50: 4 μM

98%
Desloratadine ++

Histamine H1 receptor, IC50: 51 nM

98%
Doxylamine succinate 99%
Ebastine 98%
Tripelennamine HCl +

H1 receptor, IC50: 30 μM

98%
Meclizine dihydrochloride 98%
Chlorpheniramine maleate +++

Histamine H1 receptor, IC50: 12 nM

99%
Diphenhydramine HCl 99%
Alcaftadine ++++

H1 receptor, pKi: 8.5

++

H2 receptor, pKi: 7.2

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 99%
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%
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
  • Histamine receptor

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]. The treatment with the use of the combination of azelastine hydrochloride and mometasone furoate resulted in a more pronounced alleviation of rhinological symptoms and improvement of the quality of life at the early stages of therapy in comparison with mometasone furoate monotherapy[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

Azelastine HCl 实验方案

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

CAS号79307-93-0
分子式C22H25Cl2N3O
分子量 418.359
别名 氮卓斯汀盐酸盐 ;Azelastine (hydrochloride);Azelastine hydrochloride;Azeptin;Rhinolast;Allergodil;Optivar;Astelin
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Keep in dark place,Inert atmosphere,Room temperature

溶解度

DMSO: 50 mg/mL(119.51 mM),配合低频超声助溶,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

H2O: 6.5 mg/mL(15.54 mM),配合低频超声助溶

动物实验配方
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