(R)-Cetirizine (hydrochloride) (Synonyms: Levocetirizine) |
Catalog No.GC41715
One-Click Copy Product Info
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(R)-Cetirizine (hydrochloride) is a selective, potent, oral histamine H1 receptor antagonist.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 130018-87-0
Sample solution is provided at 25 µL, 10mM.
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(R)-Cetirizine (hydrochloride) is a selective, potent, oral histamine H1 receptor antagonist[1]. (R)-Cetirizine inhibits eosinophil transendothelial migration through monolayers of human dermal or lung microvascular endothelial cells, increases the release of the metalloproteinase MMP-9, and suppresses NF-κB activation as well as ICAM-1 expression[2]. (R)-Cetirizine has been extensively used to alleviate cutaneous histamine-induced itching and the wheal and flare reaction[3].
In vitro, (R)-Cetirizine treatment (50nM) for 48 hours significantly reduced the expression levels of IL-6 and IL-8 mRNA as well as the expression level of TLR3 protein in human rhinovirus (HRV)-infected primary human nasal epithelial cells (HNECs), and prevented HRV replication[4]. 1µM of (R)-Cetirizine incubation for 24 hours effectively reduced histamine-induced VCAM-1 expression in primary nasal polyp tissue-derived fibroblasts[5].
In vivo, (R)-Cetirizine treatment via oral administration at a dose of 0.5mg/kg/day for 8 weeks improved renal function, alleviated renal oxidative stress, and mitigated aortic vascular dysfunction in diabetic rats[6]. At 6 hours after ovalbumin exposure, (R)-Cetirizine (0.020%) was administered via eye drops at 10µl every 6 hours for 24 hours, followed by 10µl every 12 hours for 2 days, and this regimen increased systemic IL-10 secretion, reduced the expression of TNF-α and TGF-β in the conjunctiva, and induced the production of Treg cells in a mouse model of type I allergic conjunctivitis[7]. Oral administration of (R)-Cetirizine at a dose of 0.5mg/kg/day for 8 weeks alleviated high-fructose diet-induced insulin resistance, ameliorated vascular dysfunction, and inhibited hepatic steatosis in rats[8].
References:
[1] Chen C. Physicochemical, pharmacological and pharmacokinetic properties of the zwitterionic antihistamines cetirizine and levocetirizine[J]. Current medicinal chemistry, 2008, 15(21): 2173-2191.
[2] Walsh G M. The anti-inflammatory effects of levocetirizine-are they clinically relevant or just an interesting additional effect?[J]. Allergy, Asthma & Clinical Immunology, 2009, 5(1): 14.
[3] Walsh G M. A review of the role of levocetirizine as an effective therapy for allergic disease[J]. Expert opinion on pharmacotherapy, 2008, 9(5): 859-867.
[4] Jang Y J, Wang J H, Kim J S, et al. Levocetirizine inhibits rhinovirus-induced ICAM-1 and cytokine expression and viral replication in airway epithelial cells[J]. Antiviral research, 2009, 81(3): 226-233.
[5] Petecchia L, Serpero L, Silvestri M, et al. The histamine-induced enhanced expression of vascular cell adhesion molecule-1 by nasal polyp-derived fibroblasts is inhibited by levocetirizine[J]. American journal of rhinology, 2006, 20(5): 445-449.
[6] Anbar H S, Shehatou G S G, Suddek G M, et al. Comparison of the effects of levocetirizine and losartan on diabetic nephropathy and vascular dysfunction in streptozotocin-induced diabetic rats[J]. European Journal of Pharmacology, 2016, 780: 82-92.
[7] García-Zepeda S, Estrada-Muñiz E, Elizondo G, et al. Levocetirizine inhibits migration of immune cells to lymph nodes and induces Treg cells in a murine type I allergic conjunctivitis model[J]. The Open Ophthalmology Journal, 2012, 6: 129.
[8] Shawky N M, Shehatou G S G, Rahim M A, et al. Levocetirizine ameliorates high fructose diet-induced insulin resistance, vascular dysfunction and hepatic steatosis in rats[J]. European journal of pharmacology, 2014, 740: 353-363.
| Cell experiment [1]: | |
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Cell lines |
A549 cells |
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Preparation Method |
A549 cells were cultured in F-12K medium supplemented with 2mM L-glutamine, 1.5g/L sodium bicarbonate, 100U/ml penicillin, 100ug/ml streptomycin, and 10% fetal bovine serum, at 37°C in an incubator with 5% CO2. A549 cells were plated at a density of 2×105 cells per well in 12-well plastic tissue culture plates. The cells were infected with HRV-16 stock at a multiplicity of infection (MOI) of 1. After adsorption for 4h at 33°C, the viral solution was removed, and the cells were rinsed with treated with 50nM (R)-Cetirizine and incubated at 33 °C for 48h. The expression levels of ICAM-1 and TLR3 were measured by flow cytometry, immunoreactive IL-6 and IL-8 were quantified using dual-antibody ELISA. |
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Reaction Conditions |
50nM; 48h |
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Applications |
(R)-Cetirizine reduced levels of ICAM-1, TLR3, IL-6 and IL-8 in HRV-infected A549 cells. |
| Animal experiment [2]: | |
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Animal models |
Male Sprague Dawley rats |
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Preparation Method |
Male Sprague Dawley rats (190-210g) were kept at constant environmental and nutritional conditions at room temperature with a 12h/12h light/dark cycle and allowed free access to standard laboratory food and water throughout the experiment. Diabetes was induced by a single intraperitoneal injection of Streptozotocin (50mg/kg) in sterile saline. Two weeks after diabetes induction, diabetic rats were randomly divided into three groups of eight rats, which received either 0.5% carboxymethyl cellulose (CMC) (3ml/kg/day; orally) [diabetic control], losartan (25mg/kg/day in 0.5% CMC; orally) or (R)-Cetirizine (0.5mg/kg/day in 0.5% CMC; orally) for eight weeks. The kidney and aorta tissues in rats were collected for analysis. |
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Dosage form |
0.5mg/kg/day; 8 weeks; p.o. |
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Applications |
(R)-Cetirizine treatment ameliorated diabetic nephropathy and aortic dysfunction in diabetic rats. |
References: [1] Jang Y J, Wang J H, Kim J S, et al. Levocetirizine inhibits rhinovirus-induced ICAM-1 and cytokine expression and viral replication in airway epithelial cells[J]. Antiviral research, 2009, 81(3): 226-233. [2] Anbar H S, Shehatou G S G, Suddek G M, et al. Comparison of the effects of levocetirizine and losartan on diabetic nephropathy and vascular dysfunction in streptozotocin-induced diabetic rats[J]. European Journal of Pharmacology, 2016, 780: 82-92. | |
| Cas No. | 130018-87-0 | SDF | |
| Synonyms | Levocetirizine | ||
| Canonical SMILES | ClC1=CC=C([C@H](N2CCN(CCOCC(O)=O)CC2)C3=CC=CC=C3)C=C1.Cl.Cl | ||
| Formula | C21H25ClN2O3•2HCl | M.Wt | 461.8 |
| Solubility | DMF: 3 mg/ml,DMSO: 12 mg/ml,PBS (pH 7.2): 10 mg/ml | Storage | 4°C, protect from light |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.1654 mL | 10.8272 mL | 21.6544 mL |
| 5 mM | 433.1 μL | 2.1654 mL | 4.3309 mL |
| 10 mM | 216.5 μL | 1.0827 mL | 2.1654 mL |
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μL
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >99.50% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 15 reference(s) in Google Scholar.)