Cat. No.: HY-17042

Cetirizine

3 Cited Publications

Customer Review

Based on 3 publication(s) in Google Scholar

Cetirizine, a second-generation antihistamine and the carboxylated metabolite of hydroxyzine, is a specific, orally active and long-acting histamine H1-receptor antagonist. Cetirizine marks antiallergic properties and inhibits eosinophil chemotaxis during the allergic response.

For research use only. We do not sell to patients.

Purity: 99.79%
CAS No.: 83881-51-0
Formula: C₂₁H₂₅ClN₂O₃
Molecular Weight:388.89

Storage:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Cetirizine Chemical Structure

CAS No.: 83881-51-0

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (3)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

All Histamine Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
HEK293	IC₅₀	>30 μM Compound: 44, Cetirizine	Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay	[PMID: 16931010]
HEK293	IC₅₀	>500 μM Compound: cetirizine	Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay Inhibition of human MATE1-mediated ASP+ uptake expressed in HEK293 cells after 1.5 mins by fluorescence assay	[PMID: 23241029]
Huh-7	CC₅₀	>100 μM Compound: Rac-3	Cytotoxicity against human Huh7.5.1 cells assessed as ATP level by luminescence analysis Cytotoxicity against human Huh7.5.1 cells assessed as ATP level by luminescence analysis	[PMID: 26599718]

In Vitro

Cetirizine (>5 μM) at higher concentrations can reduce the release of GM-CSF and IL-8 from A549 cells stimulated with IL-1β. Cetirizine exerts anti-inflammatory effects beyond histamine H1-receptor antagonist^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

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%.

In Vivo

Cetirizine (20 mg/kg, mice, orally) exerts its anti-inflammatory effects by inhibiting MIF as well as IL-8 production in mice immunized and challenged with ragweed pollen^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Male 8-week-old BALB/c mice (25-30 g) immunized and challenged with ragweed pollen^{[3]^.}

Dosage:

2 or 20 mg/kg.

Administration:

Orally, diluted in sterile water on days 18, 19, and 20.

Result:

The neutrophilia at 8 h and eosinophilia at 24 h induced by ragweed pollen extract per os were significantly reduced in the mice treated with 20 mg/kg. The dosage with 2 mg/kg had no effect.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 83881-51-0
Appearance Solid
Molecular Weight 388.89
Formula C₂₁H₂₅ClN₂O₃
Color Off-white to light yellow
SMILES

O=C(O)COCCN1CCN(C(C2=CC=C(Cl)C=C2)C3=CC=CC=C3)CC1
Structure Classification
- Ketones, Aldehydes, Acids
Initial Source
- Endogenous metabolite
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (3)

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Journal Impact Factor

Pharmacol Res

Sinomenine-induced histamine release-like anaphylactoid reactions are blocked by tranilast via inhibiting NF-κB signaling. [Abstract]

2017 Nov;125(Pt B):150-160. PMID: 28867637
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Behav Brain Res

Differential roles of prelimbic and anterior cingulate cortical region in the modulation of histaminergic and non-histaminergic itch. [Abstract]

2021 Aug 6:411:113388. PMID: 34052263

Solvent & Solubility

In Vitro:

DMSO : 175 mg/mL (450.00 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molarity Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

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In Vivo:

The following protocol is derived from the literature and is for reference only. It is recommended to first try a small sample.

Protocol 1

Cetirizine is dissolved in PBS^[6].

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (273 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

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. [Content Brief]

[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. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.5714 mL	12.8571 mL	25.7142 mL	64.2855 mL
	5 mM	0.5143 mL	2.5714 mL	5.1428 mL	12.8571 mL
	10 mM	0.2571 mL	1.2857 mL	2.5714 mL	6.4286 mL
	15 mM	0.1714 mL	0.8571 mL	1.7143 mL	4.2857 mL
	20 mM	0.1286 mL	0.6429 mL	1.2857 mL	3.2143 mL
	25 mM	0.1029 mL	0.5143 mL	1.0286 mL	2.5714 mL
	30 mM	0.0857 mL	0.4286 mL	0.8571 mL	2.1429 mL
	40 mM	0.0643 mL	0.3214 mL	0.6429 mL	1.6071 mL
	50 mM	0.0514 mL	0.2571 mL	0.5143 mL	1.2857 mL
	60 mM	0.0429 mL	0.2143 mL	0.4286 mL	1.0714 mL
	80 mM	0.0321 mL	0.1607 mL	0.3214 mL	0.8036 mL
	100 mM	0.0257 mL	0.1286 mL	0.2571 mL	0.6429 mL

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Cetirizine

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Publications Citing Use of MedChemExpress (MCE) Cetirizine

All Histamine Receptor Isoforms

Biological Activity

Chemical Information

Publications (3)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Cetirizine Related Classifications

Cat. No.: HY-17042