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MedKoo Cat#: 317500 | Name: Cetirizine Hydrochloride
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Cetirizine hydrochloride is a potent second-generation histamine H1 antagonist that is effective in the treatment of allergic rhinitis, chronic urticaria, and pollen-induced asthma. Cetirizine hydrochloride is a carboxylated metabolite of hydroxyzine that acts as a selective Histamine H1 receptor inverse agonist. Compared to its parent compound, it shows similar antihistaminic activity, but with greater H1 selectivity and less sedative effects.

Chemical Structure

Cetirizine Hydrochloride
Cetirizine Hydrochloride
CAS#83881-52-1 (HCl)

Theoretical Analysis

MedKoo Cat#: 317500

Name: Cetirizine Hydrochloride

CAS#: 83881-52-1 (HCl)

Chemical Formula: C21H27Cl3N2O3

Exact Mass: 0.0000

Molecular Weight: 461.81

Elemental Analysis: C, 54.62; H, 5.89; Cl, 23.03; N, 6.07; O, 10.39

Price and Availability

Size Price Availability Quantity
1g USD 90.00 Ready to ship
2g USD 150.00 Ready to ship
5g USD 250.00 2 weeks
10g USD 425.00 2 weeks
25g USD 850.00 2 Weeks
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Related CAS #
83881-51-0 (free base) 83881-52-1 (HCl)
Synonym
Cetirizine Hydrochloride; 83881-52-1; Reactine; Zyrtec; CETIRIZINE HYDROCHLORIDE; Alerlisin; Aliud Brand of Cetirizine Dihydrochloride; Alpharma Brand of Cetirizine Dihydrochloride; AWD.pharma Brand of Cetirizine Dihydrochloride; Azupharma Brand of Cetirizine Dihydrochloride; Basics Brand of Cetirizine Dihydrochloride;
IUPAC/Chemical Name
2-[2-[4-[(4-chlorophenyl)-phenylmethyl]piperazin-1-yl]ethoxy]acetic acid;dihydrochloride
InChi Key
PGLIUCLTXOYQMV-UHFFFAOYSA-N
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
SMILES Code
C1CN(CCN1CCOCC(=O)O)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl.Cl.Cl
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Product Data
Product Data
Certificate of Analysis
View CoA: current batch, Lot#C20M02C17
Safety Data Sheet (SDS)
View Safety Data Sheet (SDS)
Instruction
View handling instruction
Biological target:
Cetirizine dihydrochloride is a long-acting histamine H1-receptor antagonist.
In vitro activity:
To assess the impact of cetirizine treatment on the function of P-gp as an efflux pump in vitro, this study examined the P-gp-mediated Rho123 transport in Caco-2 cells treated with cetirizine using verapamil as a P-gp inhibitor. As shown in Figure 4, 100 µM cetirizine significantly increased the intracellular accumulation of Rho123 in Caco-2 cells (p < 0.05). The mean intracellular concentration of Rho123 in control cells was 50.2 ± 6.0, while in cetirizine and verapamil treated cells were 88.8 ± 2.3 and 420.6 ± 25.4 pg/mg protein, respectively. Reference: Adv Pharm Bull. 2016 Mar; 6(1): 111–118. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4845543/
In vivo activity:
The H1-receptor antagonist cetirizine was given to C57BL/6 mice in the drinking water at 25 mg/kg/day, to determine whether high-fat diet (HFD)-induced glucose intolerance is affected. The non-fasting blood glucose levels of HFD mice were higher than those of ND mice after 7 weeks of diet (Figure 3). A 1-week treatment with cetirizine resulted in a normalization of the blood glucose levels of HFD mice (Figure 3). Cetirizine did not affect the blood glucose concentrations of ND mice (Figure 3). Reference: Ups J Med Sci. 2015 Mar; 120(1): 40–46. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4389006/
Solvent mg/mL mM
Solubility
DMSO 62.6 135.45
DMF 3.0 6.50
PBS (pH 7.2) 10.0 21.65
Water 79.4 171.91
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 461.81 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Mesgari Abbasi M, Valizadeh H, Hamishekar H, Mohammadnejad L, Zakeri-Milani P. The Effects of Cetirizine on P-glycoprotein Expression and Function In vitro and In situ. Adv Pharm Bull. 2016 Mar;6(1):111-8. doi: 10.15171/apb.2016.017. Epub 2016 Mar 17. PMID: 27123426; PMCID: PMC4845543. 2. Anvari E, Fred RG, Welsh N. The H1-receptor antagonist cetirizine protects partially against cytokine- and hydrogen peroxide-induced β-TC6 cell death in vitro. Pancreas. 2014 May;43(4):624-9. doi: 10.1097/MPA.0000000000000076. PMID: 24717804. 3. Hwang S, Chung CJ, Choi YJ, Kim T, Kim KH. The effect of cetirizine, a histamine 1 receptor antagonist, on bone remodeling after calvarial suture expansion. Korean J Orthod. 2020 Jan;50(1):42-51. doi: 10.4041/kjod.2020.50.1.42. Epub 2020 Jan 22. PMID: 32042719; PMCID: PMC6995828. 4. Anvari E, Wang X, Sandler S, Welsh N. The H1-receptor antagonist cetirizine ameliorates high-fat diet-induced glucose intolerance in male C57BL/6 mice, but not diabetes outcome in female non-obese diabetic (NOD) mice. Ups J Med Sci. 2015 Mar;120(1):40-6. doi: 10.3109/03009734.2014.967422. Epub 2014 Oct 7. PMID: 25291144; PMCID: PMC4389006.
In vitro protocol:
1. Mesgari Abbasi M, Valizadeh H, Hamishekar H, Mohammadnejad L, Zakeri-Milani P. The Effects of Cetirizine on P-glycoprotein Expression and Function In vitro and In situ. Adv Pharm Bull. 2016 Mar;6(1):111-8. doi: 10.15171/apb.2016.017. Epub 2016 Mar 17. PMID: 27123426; PMCID: PMC4845543. 2. Anvari E, Fred RG, Welsh N. The H1-receptor antagonist cetirizine protects partially against cytokine- and hydrogen peroxide-induced β-TC6 cell death in vitro. Pancreas. 2014 May;43(4):624-9. doi: 10.1097/MPA.0000000000000076. PMID: 24717804.
In vivo protocol:
1. Hwang S, Chung CJ, Choi YJ, Kim T, Kim KH. The effect of cetirizine, a histamine 1 receptor antagonist, on bone remodeling after calvarial suture expansion. Korean J Orthod. 2020 Jan;50(1):42-51. doi: 10.4041/kjod.2020.50.1.42. Epub 2020 Jan 22. PMID: 32042719; PMCID: PMC6995828. 2. Anvari E, Wang X, Sandler S, Welsh N. The H1-receptor antagonist cetirizine ameliorates high-fat diet-induced glucose intolerance in male C57BL/6 mice, but not diabetes outcome in female non-obese diabetic (NOD) mice. Ups J Med Sci. 2015 Mar;120(1):40-6. doi: 10.3109/03009734.2014.967422. Epub 2014 Oct 7. PMID: 25291144; PMCID: PMC4389006.
1: Preis M, Grother L, Axe P, Breitkreutz J. In-vitro and in-vivo evaluation of taste-masked cetirizine hydrochloride formulated in oral lyophilisates. Int J Pharm. 2015 Aug 1;491(1-2):8-16. doi: 10.1016/j.ijpharm.2015.06.002. Epub 2015 Jun 5. PubMed PMID: 26051543. 2: Sharma D, Singh G, Kumar D, Singh M. Formulation development and evaluation of fast disintegrating tablets of salbutamol sulphate, cetirizine hydrochloride in combined pharmaceutical dosage form: a new era in novel drug delivery for pediatrics and geriatrics. J Drug Deliv. 2015;2015:640529. doi: 10.1155/2015/640529. Epub 2015 Feb 25. PubMed PMID: 25810924; PubMed Central PMCID: PMC4355560. 3: El-Say KM, El-Helw AR, Ahmed OA, Hosny KM, Ahmed TA, Kharshoum RM, Fahmy UA, Alsawahli M. Statistical optimization of controlled release microspheres containing cetirizine hydrochloride as a model for water soluble drugs. Pharm Dev Technol. 2015;20(6):738-46. doi: 10.3109/10837450.2014.920353. Epub 2014 May 26. PubMed PMID: 24856961. 4: Sharma D, Singh M, Kumar D, Singh G. Formulation Development and Evaluation of Fast Disintegrating Tablet of Cetirizine Hydrochloride: A Novel Drug Delivery for Pediatrics and Geriatrics. J Pharm (Cairo). 2014;2014:808167. doi: 10.1155/2014/808167. Epub 2014 Feb 18. PubMed PMID: 26556203; PubMed Central PMCID: PMC4590798. 5: Wildermuth K, Zabel S, Rosychuk RA. The efficacy of cetirizine hydrochloride on the pruritus of cats with atopic dermatitis: a randomized, double-blind, placebo-controlled, crossover study. Vet Dermatol. 2013 Dec;24(6):576-81, e137-8. doi: 10.1111/vde.12067. Epub 2013 Sep 20. PubMed PMID: 24112588. 6: Tsunemi Y, Saeki H, Tamaki K, Sato S, Nakamura K. Cetirizine hydrochloride suppresses the CCL17 production of epidermal keratinocytes and dermal fibroblasts. Int J Dermatol. 2012 Aug;51(8):1003-5. doi: 10.1111/j.1365-4632.2010.04708.x. PubMed PMID: 22788822. 7: Griffin JS, Scott DW, Miller WH Jr, Tranchina MM. An open clinical trial on the efficacy of cetirizine hydrochloride in the management of allergic pruritus in cats. Can Vet J. 2012 Jan;53(1):47-50. PubMed PMID: 22753962; PubMed Central PMCID: PMC3239147. 8: Trivedi RK, Patel MC, Jadhav SB. A Rapid, Stability Indicating RP-UPLC Method for Simultaneous Determination of Ambroxol Hydrochloride, Cetirizine Hydrochloride and Antimicrobial Preservatives in Liquid Pharmaceutical Formulation. Sci Pharm. 2011 Sep;79(3):525-43. doi: 10.3797/scipharm.1103-19. Epub 2011 May 26. PubMed PMID: 21886901; PubMed Central PMCID: PMC3163363. 9: Okubo Y, Shigoka Y, Yamazaki M, Tsuboi R. Double dose of cetirizine hydrochloride is effective for patients with urticaria resistant: a prospective, randomized, non-blinded, comparative clinical study and assessment of quality of life. J Dermatolog Treat. 2013 Apr;24(2):153-60. doi: 10.3109/09546634.2011.608783. Epub 2011 Aug 24. PubMed PMID: 21810005. 10: Sun Y, Jiang Y, An K. Preparation and the influencing factors of cetirizine hydrochloride microemulsion. Artif Cells Blood Substit Immobil Biotechnol. 2011 Jun;39(3):174-6. doi: 10.3109/10731199.2010.525710. Epub 2010 Oct 15. PubMed PMID: 20946090. 11: Xu FG, Liu Y, Zhang ZJ, Tian Y, Chen Y. Pharmacokinetics and bioequivalence study of two cetirizine hydrochloride formulations in healthy Chinese male volunteers. Arzneimittelforschung. 2009;59(9):440-4. doi: 10.1055/s-0031-1296422. PubMed PMID: 19856790. 12: Tashiro M, Kato M, Miyake M, Watanuki S, Funaki Y, Ishikawa Y, Iwata R, Yanai K. Dose dependency of brain histamine H(1) receptor occupancy following oral administration of cetirizine hydrochloride measured using PET with [11C]doxepin. Hum Psychopharmacol. 2009 Oct;24(7):540-8. doi: 10.1002/hup.1051. PubMed PMID: 19697300. 13: Sugiura K, Hirai S, Suzuki T, Usuda T, Kondo T, Azumi T, Masaki S, Yokoi T, Nitta Y, Kamiya S, Ando K, Mori T, Tomita Y. Evaluation of cetirizine hydrochloride-based therapeutic strategy for chronic urticaria. Nagoya J Med Sci. 2008 Aug;70(3-4):97-106. PubMed PMID: 18954028. 14: Bhatia NM, Ganbavale SK, Bhatia MS, More HN, Kokil SU. RP-HPLC and Spectrophotometric Estimation of Ambroxol Hydrochloride and Cetirizine Hydrochloride in Combined Dosage Form. Indian J Pharm Sci. 2008 Sep;70(5):603-8. doi: 10.4103/0250-474X.45398. PubMed PMID: 21394256; PubMed Central PMCID: PMC3038284. 15: Liu JY, Zhao YZ, Peng C, Li FQ, Zhu QG, Hu JH. [Effect of cetirizine hydrochloride on the expression of substance P receptor and cytokines production in human epidermal keratinocytes and dermal fibroblasts]. Yao Xue Xue Bao. 2008 Apr;43(4):383-7. Chinese. PubMed PMID: 18664200. 16: Enomoto T, Ide T, Ogino S. Construction of an environmental exposure unit and investigation of the effects of cetirizine hydrochloride on symptoms of cedar pollinosis in Japan. J Investig Allergol Clin Immunol. 2007;17(3):173-81. PubMed PMID: 17583105. 17: Gowekar NM, Pande VV, Kasture AV, Tekade AR, Chandorkar JG. Spectrophotometric estimation of ambroxol and cetirizine hydrochloride from tablet dosage form. Pak J Pharm Sci. 2007 Jul;20(3):250-1. PubMed PMID: 17545112. 18: Liu JY, Hu JH, Zhu QG, Li FQ, Sun HJ. [Effect of cetirizine hydrochloride on the expression of substance P in IgE-mediated triphasic cutaneous reaction]. Yao Xue Xue Bao. 2005 Jul;40(7):649-53. Chinese. PubMed PMID: 16196274. 19: Ousler GW, Wilcox KA, Gupta G, Abelson MB. An evaluation of the ocular drying effects of 2 systemic antihistamines: loratadine and cetirizine hydrochloride. Ann Allergy Asthma Immunol. 2004 Nov;93(5):460-4. PubMed PMID: 15562885. 20: Li Q, Shen WB, Zou QG. [NMR studies on cetirizine hydrochloride]. Yao Xue Xue Bao. 2003 Oct;38(10):767-70. Chinese. PubMed PMID: 14730901.

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