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

货号:A930064 同义名: 盐酸左旋西替利嗪 / (R)-Cetirizine dihydrochloride; Xyzal

Levocetirizine 2HCl是一种第三代非镇静抗组胺药,是第二代抗组胺药 cetirizine 的衍生物。

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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/左西替利嗪二盐酸盐 化学结构 CAS号:130018-87-0
Levocetirizine 2HCl/左西替利嗪二盐酸盐 化学结构
CAS号:130018-87-0
Levocetirizine 2HCl/左西替利嗪二盐酸盐 3D分子结构
CAS号:130018-87-0
Levocetirizine 2HCl/左西替利嗪二盐酸盐 化学结构 CAS号:130018-87-0
Levocetirizine 2HCl/左西替利嗪二盐酸盐 3D分子结构 CAS号:130018-87-0
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Levocetirizine 2HCl/左西替利嗪二盐酸盐 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 2HCl 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 96%
Betahistine +

Histamine H3 receptor, IC50: 1.9 μM

99%
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

99%
Azelastine HCl 98%
Epinastine HCl 99%
Levodropropizine 97%
Cyproheptadine HCl 98%
Hesperetin 97%
Olopatadine HCl 98%
Mianserin HCl 99+%
Buclizine 2HCl 95%
Latrepirdine 2HCl GluR 99%
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/左西替利嗪二盐酸盐 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/左西替利嗪二盐酸盐 动物实验

Species
Animal Model
Administration Dosage Frequency Description References
Children Patients with allergic rhinitis Oral 5 mg Once every evening for 4 weeks To evaluate the safety and efficacy of levocetirizine and montelukast combination therapy in children with allergic rhinitis. Results showed that combination therapy was more effective than monotherapy in reducing both daytime and nighttime nasal symptoms. Allergy Asthma Immunol Res. 2024 Nov;16(6):652-667
Mice Parkinson's disease model Oral 0.5 and 1 mg/kg Once daily for 23 days To evaluate the effects of Levocetirizine on behavioral and biochemical parameters in a Parkinson's disease model in mice. Results showed that Levocetirizine significantly improved motor coordination, reduced catalepsy, and enhanced antioxidant enzyme activities. ACS Omega. 2022 Apr 20;7(17):14772-14783
Wistar rats Atopic dermatitis and MRSA skin infection model Topical administration 7.5 mg LVC 1 day Evaluate the deposition and safety of levocetirizine in the skin Pharmaceuticals (Basel). 2025 Apr 27;18(5):633
Male Wistar rats Alopecia model Topically 2.5 mg/mL Single dose, duration of 10 hours To evaluate the skin deposition of LVC from CCPCs, results showed that the AUC0-10 of the CCPCs group was significantly higher than that of the LVC solution group, indicating increased LVC deposition in the skin. Drug Deliv. 2022 Dec;29(1):2784-2795

Levocetirizine 2HCl/左西替利嗪二盐酸盐 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/左西替利嗪二盐酸盐 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/左西替利嗪二盐酸盐 技术信息

CAS号130018-87-0
分子式C21H27Cl3N2O3
分子量 461.81
SMILES Code O=C(O)COCCN1CCN([C@@H](C2=CC=C(Cl)C=C2)C3=CC=CC=C3)CC1.[H]Cl.[H]Cl
MDL No. MFCD07366507
别名 盐酸左旋西替利嗪 ;(R)-Cetirizine dihydrochloride; Xyzal; Xusal; UCB 28556; (-)-Cetirizine; Levocetirizine; (-)-Cetirizine Dihydrochloride; Xyzal Dihydrochloride; Levocetirizine dihydrochloride
运输蓝冰
InChI Key PGLIUCLTXOYQMV-GHVWMZMZSA-N
Pubchem ID 9955977
存储条件

In solvent -20°C: 3-6个月 -80°C: 12个月

Pure form Keep in dark place,Sealed in dry,2-8°C

溶解方案

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

请根据您的动物给药指南选择适当的溶解方案。
以下溶解方案都请先按照体外实验的方式配制澄清的储备液,再依次添加助溶剂:
——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议现用现配,当天使用; 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
方案 二
方案 三
配制的工作液建议现用现配,短期内尽快用完。 以下溶剂前显示的百分比是指该溶剂在终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶
方案 一
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