产品说明书

Levocetirizine 2HCl

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Chemical Structure| 130018-87-0 同义名 : (R)-Cetirizine dihydrochloride;(R)-Cetirizine (hydrochloride);Xyzal;Xusal;UCB 28556;(-)-Cetirizine;Levocetirizine;(-)-Cetirizine Dihydrochloride;Xyzal Dihydrochloride;Levocetirizine dihydrochloride
CAS号 : 130018-87-0
货号 : A930064
分子式 : C21H27Cl3N2O3
纯度 : 98%
分子量 : 461.81
MDL号 : MFCD07366507
存储条件:

粉末 Inert atmosphere,Room Temperature

液体 -20°C:3-6个月-80°C:12个月

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:
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].
实验方案
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

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