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左西替利嗪二盐酸盐 /Levocetirizine 2HCl {[allProObj[0].p_purity_real_show]}

货号:A930064 同义名: (R)-Cetirizine dihydrochloride;(R)-Cetirizine (hydrochloride)

Levocetirizine 2HCl is a third-generation non-sedative antihistamine, developed from the second-generation antihistamine cetirizine.

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Type HazMat fee for 500 gram (Estimated)
Excepted Quantity USD 0.00
Limited Quantity USD 15-60
Inaccessible (Haz class 6.1), Domestic USD 80+
Inaccessible (Haz class 6.1), International USD 150+
Accessible (Haz class 3, 4, 5 or 8), Domestic USD 100+
Accessible (Haz class 3, 4, 5 or 8), International USD 200+
Levocetirizine 2HCl 化学结构 CAS号:130018-87-0
Levocetirizine 2HCl 化学结构
CAS号:130018-87-0
Levocetirizine 2HCl 3D分子结构
CAS号:130018-87-0
Levocetirizine 2HCl 化学结构 CAS号:130018-87-0
Levocetirizine 2HCl 3D分子结构 CAS号:130018-87-0
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Levocetirizine 2HCl 纯度/质量文件 产品仅供科研

货号:A930064 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 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%
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。

Levocetirizine 2HCl 生物活性

描述 Levocetirizine 2HCl ((R)-Cetirizine dihydrochloride) is a third-generation peripheral H1-receptor antagonist. Levocetirizine dihydrochloride is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine dihydrochloride has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[3]. Levocetirizine has modest sedative effects with a risk ratio of 1.67 when compared with placebo[4]. Montelukast, levocetirizine and their combination is equally effective in controlling symptoms, of allergic rhinitis[5]. Male Sprague Dawley rats received either levocetirizine (1 mg/kg/day, orally) or the vehicle of the drug (2 ml/kg/day, orally) for 1 week before a single IP injection of LPS (7.5 mg/kg). Levocetirizine attenuated lung edema and mitigated the increases in BALF (bronchoalveolar lavage fluid) protein levels, LDH (lactate dehydrogenase) activity, and lung leukocyte recruitment in LPS-challenged rats. Additionally, TNF-α protein levels in BALF and lung tissue were diminished by levocetirizine administration. Levocetirizine may offer protection against lung tissue damage and inflammation in LPS-challenged rats[6].

Levocetirizine 2HCl 参考文献

[1]Hampel F, Ratner P, et al. Safety and tolerability of levocetirizine dihydrochloride in infants and children with allergic rhinitis or chronic urticaria. Allergy Asthma Proc. 2010 Jul-Aug;31(4):290-5.

[2]Liu X, Du Y, et al. Study on the interaction of levocetirizine dihydrochloride with human serum albumin by molecular spectroscopy. Spectrochim Acta A Mol Biomol Spectrosc. 2009 Dec;74(5):1189-96.

[3]Johnson M, Kwatra G, Badyal DK, Thomas EA. Levocetirizine and rupatadine in chronic idiopathic urticaria. Int J Dermatol. 2015 Oct;54(10):1199-204

[4]Snidvongs K, Seresirikachorn K, Khattiyawittayakun L, Chitsuthipakorn W. Sedative Effects of Levocetirizine: A Systematic Review and Meta-Analysis of Randomized Controlled Studies. Drugs. 2017 Feb;77(2):175-186

[5]Andhale S, Goel HC, Nayak S. Comparison of Effect of Levocetirizine or Montelukast Alone and in Combination on Symptoms of Allergic Rhinitis. Indian J Chest Dis Allied Sci. 2016 Apr-Jun;58(2):103-5

[6]Fahmi ANA, Shehatou GSG, Salem HA. Levocetirizine Pretreatment Mitigates Lipopolysaccharide-Induced Lung Inflammation in Rats. Biomed Res Int. 2018 Aug 13;2018:7019759

Levocetirizine 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

Levocetirizine 2HCl 技术信息

CAS号130018-87-0
分子式C21H27Cl3N2O3
分子量 461.81
别名 (R)-Cetirizine dihydrochloride;(R)-Cetirizine (hydrochloride);Xyzal;Xusal;UCB 28556;(-)-Cetirizine;Levocetirizine;(-)-Cetirizine Dihydrochloride;Xyzal Dihydrochloride;Levocetirizine 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

DMSO: 105 mg/mL(227.37 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: 100 mg/mL(216.54 mM),配合低频超声助溶

动物实验配方
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