Home Neuronal Signaling Histamine Receptor antagonist Levocetirizine Dihydrochloride

research use only

Levocetirizine Dihydrochloride Histamine Receptor antagonist

Cat.No.S4849

Levocetirizine (Xyzal, (-)-Cetirizine) is the active R-enantiomer of cetirizine and represents a new second-generation histamine H1 antagonist.
Levocetirizine Dihydrochloride Histamine Receptor antagonist Chemical Structure

Chemical Structure

Molecular Weight: 461.81

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S484901 DMSO]92 mg/mL]false]Water]92 mg/mL]false]Ethanol]7 mg/mL]false Purity: 99.86%
99.86

Chemical Information, Storage & Stability

Molecular Weight 461.81 Formula

C21H25ClN2O3.2HCl

 Storage (From the date of receipt)
CAS No. 130018-87-0 -- Storage of Stock Solutions

Synonyms Xyzal Dihydrochloride, (-)-Cetirizine Dihydrochloride Smiles C1CN(CCN1CCOCC(=O)O)C(C2=CC=CC=C2)C3=CC=C(C=C3)Cl.Cl.Cl

Solubility

In vitro
Batch:

DMSO : 92 mg/mL (199.21 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 92 mg/mL

Ethanol : 7 mg/mL

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
Batch:

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg g μL

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Mechanism of Action

Targets/IC50/Ki
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].
References

Tech Support

Handling Instructions

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

Please enter your name.
Please enter your email. Please enter a valid email address.
Please write something to us.

Signaling Pathway Map