2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Cetirizine

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.

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No. CAS : 83881-51-0

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Based on 3 publication(s) in Google Scholar

Other Forms of Cetirizine:

Cetirizine Related Antibodies

Top Publications Citing Use of Products

    Cetirizine purchased from MedChemExpress. Usage Cited in: Pharmacol Res. 2017 Nov;125(Pt B):150-160.  [Abstract]

    The IL-33 production in different treatment groups is determined in rat skin by immunohistochemistry assay.

    Ver todos los productos específicos de isoformas Histamine Receptor:

    Ver todas las isoformas
    H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

    • Actividad biológica

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    • Referencias

    • Revisión del cliente

    Descripciòn

    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[1][2][3].

    Cellular Effect
    Cell Line Type Value Description References
    HEK293 IC50
    > 30 3
    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
    >30 3
    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 3
    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]
    HEK293 IC50
    >500 3
    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 3
    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]
    Huh-7 CC50
    >100 3
    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]
    HEK293 IC50
    > 30 3
    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 3
    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 3
    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.

    Cetirizine Related Antibodies
    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.
    Ensayo clínico
    Peso molecular

    388.89

    Fòrmula

    C21H25ClN2O3
    No. CAS
    Appearance

    Solid

    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
    Initial Source
    Envío

    Room temperature in continental US; may vary elsewhere.
    Almacenamiento

    4°C, protect from light

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

    Solvente y solubilidad
    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)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 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
    View the Complete Stock Solution Preparation Table

    * 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.

    • Calculadora de molaridad

    • Calculadora de dilución

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

    Mass
    =
    Concentration
    ×
    Volume
    ×
    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    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

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Calculation results:
    Working solution concentration: mg/mL
    Pureza y Documentación

    Purity: 99.74%

    SDS (393 KB)

    COA (245 KB) HNMR (265 KB) RP-HPLC (247 KB) LCMS (91 KB)

    Instrucciones de manejo (2659 KB)
    Referencias

    Complete Stock Solution Preparation Table

    * 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.

    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 Related Classifications

    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Cetirizine83881-51-0Histamine ReceptorhistamineSARARIL-1βGM-CSFIL-8SeasonalallergicrhinitisInhibitorinhibitorinhibit

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    Nombre del producto:
    Cetirizine
    Cat. No.:
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