Levocetirizine Dihydrochloride

Catalog No.S4849 Synonyms: Xyzal Dihydrochloride, (-)-Cetirizine Dihydrochloride

Levocetirizine Dihydrochloride Chemical Structure

Molecular Weight(MW): 461.81

Levocetirizine is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.

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Biological Activity

Description Levocetirizine is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.
Targets
H1 receptor [1]
()
In vitro

Levocetirizine is a selective antihistaminic that acts through H1 receptor. Levocetirizine inhibits eotaxin-induced eosinophil transendothelial migration through monolayers of human dermal or lung microvascular endothelial cells in vitro. The drug also inhibits both resting and granulocyte-macrophage colony-stimulating factor (GM-CSF)-stimulated eosinophil adhesion to vascular cell adhesion molecule-1 (VCAM-1), eotaxin production by endothelial cells and ICAM-1, as well as major histocompatability complex (MHC) class I expression by interferon (IFN)-γ-stimulated keratinocytes[1].

In vivo In vivo, levocetirizine has rapid absorption and high bioavailability, a low potential for drug interactions, low-volume distribution and a lack of effects on cognition, psychomotor function or the cardiovascular system[1]. Levocetirizine improves renal function in diabetic rat. It attenuates the elevated renal levels of TNF-α and TGF-β1, ameliorates renal oxidative stress and restores NO bioavailability in diabetic kidney. Levocetirizine elicits vasculoprotective and renoprotective effects in experimental diabetes[2].

Protocol

Animal Research:

[2]

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  • Animal Models: Male Sprague Dawley rats (with diabetes induced by STZ)
  • Formulation: 0.5% carboxymethyl cellulose
  • Dosages: 0.5 mg/kg/day
  • Administration: orally
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL (199.21 mM)
Water 92 mg/mL (199.21 mM)
Ethanol 7 mg/mL (15.15 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 461.81
Formula

C21H25ClN2O3.2ClH

CAS No. 130018-87-0
Storage powder
in solvent
Synonyms Xyzal Dihydrochloride, (-)-Cetirizine Dihydrochloride

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID