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Purity: ≥98%
Cetirizine 2HCl (P-071; UCB P071; Reactine; Zyrtec; Alerlisin; AC-170; P071), the dihydrochloride salt of cetirizine and a major active metabolite of hydroxyzine, is a 2nd-generation antihistamine used in the treatment of allergies, hay fever, angioedema, and urticarial etc. It functions as a specific inverse agonist of H1 receptor.
| Targets |
Histamine receptor
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| ln Vivo |
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| Enzyme Assay |
Cell Line: Human airway epithelial cell line A549
Concentration: 0-10 μM Incubation Time: 24 h Result: The survival of A549 cells incubated with various concentrations of cetirizine (0.1, 1, 2.5, 5, and 10 μM) for 24 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%. |
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| Animal Protocol |
Male 8-week-old BALB/c mice (25-30 g) immunized and challenged with ragweed pollen
2 or 20 mg/kg Orally, diluted in sterile water on days 18, 19, and 20. |
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| References |
| Molecular Formula |
C21H27CL3N2O3
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| Molecular Weight |
461.81
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| Exact Mass |
460.11
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| CAS # |
83881-52-1
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| Related CAS # |
Cetirizine; 83881-51-0; 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
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| Appearance |
White to off-white solid powder
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| SMILES |
C1CN(CCN1CCOCC(=O)O)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl.Cl.Cl
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| InChi Key |
PGLIUCLTXOYQMV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C21H25ClN2O3.2ClH/c22-19-8-6-18(7-9-19)21(17-4-2-1-3-5-17)24-12-10-23(11-13-24)14-15-27-16-20(25)26;;/h1-9,21H,10-16H2,(H,25,26);2*1H
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| Chemical Name |
2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]acetic acid;dihydrochloride
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| Synonyms |
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (5.41 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 120 mg/mL (259.85 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1654 mL | 10.8270 mL | 21.6539 mL | |
| 5 mM | 0.4331 mL | 2.1654 mL | 4.3308 mL | |
| 10 mM | 0.2165 mL | 1.0827 mL | 2.1654 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.
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