Cetirizine dihydrochloride

SKU: orb1223902

Description

A second-generation antihistamine that acts as a selective H1 receptor antagonist; used in the treatment of allergies.Allergy Approved(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.(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.

Images & Validation

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Key Properties

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CAS Number	83881-52-1
MW	461.8097
Purity	>98% (HPLC)
Formula	C₂₁H₂₇Cl₃N₂O₃
SMILES	Cl.OC(=O)COCCN1CCN(CC1)C(C1=CC=CC=C1)C1=CC=C(Cl)C=C1
Target	Histamine Receptor
Solubility	10 mM in DMSO

Bioactivity

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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. Animal model: Male 8-week-old BALB/c mice (25-30 g) immunized and challenged with ragweed pollen. Dosage: 2 or 20 mg/kg. Administration: Orally, diluted in sterile water on days 18, 19, and 20.

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. Cell Viability 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%.

Storage & Handling

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Storage	Storage temperature: -20°C. Stability: ≥ 2 years
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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P-071

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Gene Symbol

Histamine Receptor

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