Size | Price | Stock | Qty |
---|---|---|---|
100mg |
|
||
Other Sizes |
|
Cetirizine (Alerlisin; AC-170; P-071; UCB P071; Reactine; Zyrtec; P071), a major active metabolite of hydroxyzine, is a 2nd-generation antihistamine used in the treatment of allergies, hay fever, angioedema, and urticarial etc. It acts as a selective H1 receptor inverse agonist.
ln Vitro |
Cetirizine (>5 μM) at higher doses inhibits the release of GM-CSF and IL-8 from A549 cells treated with IL-1β. Cetirizine has anti-inflammatory properties in addition to acting as a histamine H1 receptor antagonist[2].
|
---|---|
ln Vivo |
When mice are exposed with ragweed pollen and immunized, cetirizine (20 mg/kg, mice) inhibits the production of IL-8 and MIF, hence reducing inflammation[3].
|
Cell Assay |
Cell Viability Assay[2]
Cell Types: Human airway epithelial cell line A549. Tested Concentrations: 0-10 μM. Incubation Duration: 24 h. Experimental Results: The survival of A549 cells incubated with various concentrations of cetirizine (0.1, 1, 2.5, 5, and 10 μM ) for 24 hrs (hours) were all higher than 90% when comparing with the control group by MTT test. Cetirizine, 5 and 10 μM, suppressed GM-CSF release by 70.71 and 61.55%, respectively. Preincubation with cetirizine, 10 μM, suppressed the IL -8 secretion by 75.04%. |
Animal Protocol |
Animal/Disease Models: Male 8weeks old BALB/ c mice (25-30 g) immunized and challenged with ragweed pollen[3].
Doses: 2 or 20 mg/kg. Route of Administration: Orally, diluted in sterile water on days 18, 19, and 20. Experimental Results: The neutrophilia at 8 h and eosinophilia at 24 h induced by ragweed pollen extract per os were Dramatically decreased in the mice treated with 20 mg/kg. The dosage with 2 mg/kg had no effect. |
References |
[1]. Caroline M. Spencer, et al. Cetirizine. Drugs 46 (6): 1055•1080, 1993.
[2]. Shih MY, et al. Influence of cetirizine and levocetirizine on two cytokines secretion in human airway epithelial cells. Allergy Asthma Proc. 2008 Sep-Oct;29(5):480-5. [3]. Shimizu T, et al. Cetirizine, an H1-receptor antagonist, suppresses the expression of macrophage migration inhibitory factor: its potential anti-inflammatory action. Clin Exp Allergy. 2004 Jan;34(1):103-9. |
Molecular Formula |
C21H25CLN2O3
|
---|---|
Molecular Weight |
388.888
|
CAS # |
83881-51-0
|
Related CAS # |
Cetirizine dihydrochloride;83881-52-1;Cetirizine-d4;1219803-84-5;Cetirizine-d8;774596-22-4;Levocetirizine;130018-77-8;Levocetirizine dihydrochloride;130018-87-0;Cetirizine methyl ester;83881-46-3;Cetirizine-d4 dihydrochloride;Cetirizine-d8 dihydrochloride;2070015-04-0
|
SMILES |
O=C(O)COCCN1CCN(C(C2=CC=C(Cl)C=C2)C3=CC=CC=C3)CC1
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: This product requires protection from light (avoid light exposure) during transportation and storage. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO : ~250 mg/mL (~642.86 mM)
|
---|---|
Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400  (Please use freshly prepared in vivo formulations for optimal results.) |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.5714 mL | 12.8571 mL | 25.7142 mL | |
5 mM | 0.5143 mL | 2.5714 mL | 5.1428 mL | |
10 mM | 0.2571 mL | 1.2857 mL | 2.5714 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.