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/ Cetirizine 2HCl

盐酸西替利嗪 /Cetirizine 2HCl {[allProObj[0].p_purity_real_show]}

货号：A535405 同义名： P071;Cetirizine (hydrochloride)

Cetirizine 2HCl, a metabolite of hydroxyzine, is racemic selective and inverse agonist of H1 receptor used in the treatment of allergies and hay fever.

Cetirizine 2HCl 化学结构 CAS号：83881-52-1
Cetirizine 2HCl 化学结构
CAS号：83881-52-1
Cetirizine 2HCl 3D分子结构
CAS号：83881-52-1
Cetirizine 2HCl 化学结构 CAS号：83881-52-1
Cetirizine 2HCl 3D分子结构 CAS号：83881-52-1
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Cetirizine 2HCl 纯度/质量文件 产品仅供科研

货号：A535405 标准纯度： {[allProObj[0].p_purity_real_show]}
批次查询： 批次纯度:

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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 ++

rat H3 receptor, Ki: 1.44 μM

human H3 receptor, Ki: 1.2 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。

Cetirizine 2HCl 生物活性

靶点

  • Histamine receptor
描述 Cetirizine dihydrochloride, a second-generation antihistamine and a human metabolite of hydroxyzine, is an orally-active and selective histamine H1-receptor antagonist[3]. Cetirizine exhibits high intestinal absorption in humans and its oral bioavailability is estimated to be greater than 70%[4]. Compared with the majority of other SGAHs (second-generation H1 antihistamines), cetirizine was generally shown to have a more favourable pharmacological profile, to be well tolerated, be at least equally or more efficacious in attenuating/inhibiting nasal and ocular symptoms and to improve the quality of life in AR ((allergic rhinitis) patients[5]. Cetirizine may also have a role in the treatment of certain forms of physical urticaria, atopic dermatitis and reactions to mosquito bites[6].

Cetirizine 2HCl 临床研究

NCT号 适应症或疾病 临床期 招募状态 预计完成时间 地点
NCT00628108 Allergic Rhinitis ... 展开 >> Chronic Urticaria 收起 << Phase 3 Completed - United States, Alabama ... 展开 >> Birmingham, Alabama, United States United States, Arkansas Hot Springs, Arkansas, United States Jonesboro, Arkansas, United States Little Rock, Arkansas, United States United States, California Bakersfield, California, United States Crescent City, California, United States Huntington Beach, California, United States Los Angeles, California, United States Orange, California, United States Roseville, California, United States Stockton, California, United States United States, Georgia Albany, Georgia, United States Gainesville, Georgia, United States United States, Illinois Normal, Illinois, United States United States, Missouri Bridgeton, Missouri, United States United States, Nebraska Omaha, Nebraska, United States United States, Oklahoma Oklahoma City, Oklahoma, United States United States, South Carolina Barnwell, South Carolina, United States Spartanburg, South Carolina, United States United States, Tennessee Kingsport, Tennessee, United States United States, Texas Austin, Texas, United States Dallas, Texas, United States El Paso, Texas, United States San Antonio, Texas, United States Sugarland, Texas, United States United States, Virginia Richmond, Virginia, United States 收起 <<
NCT00521131 Rhinitis Alle... 展开 >>rgic Perennial 收起 << Phase 4 Completed - -
NCT00520754 Cough Phase 2 Completed - -

Cetirizine 2HCl 参考文献

[1]Meh A, Sprogar S, et al. Effect of cetirizine, a histamine (H(1)) receptor antagonist, on bone modeling during orthodontic tooth movement in rats. Am J Orthod Dentofacial Orthop. 2011 Apr;139(4):e323-9.

[2]Naclerio RM. Additional properties of cetirizine, a new H1 antagonist. Allergy Proc. 1991 May-Jun;12(3):187-91.

[3]Portnoy JM, Dinakar C. Review of cetirizine hydrochloride for the treatment of allergic disorders. Expert Opin Pharmacother. 2004 Jan;5(1):125-35

[4]Chen C. Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine. Curr Med Chem. 2008;15(21):2173-91

[5]Zhang L, Cheng L, Hong J. The clinical use of cetirizine in the treatment of allergic rhinitis. Pharmacology. 2013;92(1-2):14-25

[6]Spencer CM, Faulds D, Peters DH. Cetirizine. A reappraisal of its pharmacological properties and therapeutic use in selected allergic disorders. Drugs. 1993 Dec;46(6):1055-80

Cetirizine 2HCl 实验方案

计算器
存储液制备 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.17mL

0.43mL

0.22mL

10.83mL

2.17mL

1.08mL

21.65mL

4.33mL

2.17mL

Cetirizine 2HCl 技术信息

CAS号83881-52-1
分子式C21H27Cl3N2O3
分子量 461.81
别名 P071;Cetirizine (hydrochloride);UCB-P 071;Cetirizine DiHCl;Cetirizine dihydrochloride
运输蓝冰
存储条件

液体 -20°C:3-6个月-80°C:12个月

粉末 Inert atmosphere,Room Temperature
溶解度
动物实验配方

Tags: Cetirizine | 83881-52-1 | P071 | P 071 | P-071 | H1-receptor Antagonist | GPCR/G Protein | Neuronal Signaling | Immunology/Inflammation | Histamine Receptor | 仅供科研使用 | AmBeed-信号通路专用抑制剂 | Cetirizine 2HCl 纯度/质量文件 | Cetirizine 2HCl 亚型比较 | Cetirizine 2HCl 生物活性 | Cetirizine 2HCl 临床数据 | Cetirizine 2HCl 参考文献 | Cetirizine 2HCl 实验方案 | Cetirizine 2HCl 技术信息

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