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Levocetirizine Dihydrochloride Histamine Receptor antagonist

Name: Levocetirizine Dihydrochloride
Brand: Selleck Chemicals
SKU: S4849
Rating: 5 (1 reviews)

Cat.No.S4849

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

Chemical Structure

Molecular Weight: 461.81

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Quality Control

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

Cited in Nature Medicine for its top-tier quality
COA
NMR
HPLC
SDS
Datasheet

99.86

Related Targets	Adrenergic Receptor AChR 5-HT Receptor COX Calcium Channel Dopamine Receptor GABA Receptor TRP Channel Cholinesterase (ChE) GluR
Other Histamine Receptor Inhibitors	GSK2879552 Dihydrochloride JNJ-7777120 Ebastine Ciproxifan Maleate Mianserin HCl Astemizole Lafutidine Mizolastine Rupatadine Fumarate Betahistine 2HCl

Chemical Information, Storage & Stability

Molecular Weight	461.81	Formula	C₂₁H₂₅ClN₂O₃.₂HCl	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	130018-87-0	--		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
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
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Dilution Calculator Molecular Weight Calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg Average weight of animals: g Dosing volume per animal:μL Number of animals:

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+ %

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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
In vitro	Levocetirizine is a selective antihistamine that acts through the 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 histocompatibility complex (MHC) class I expression by interferon (IFN)-γ-stimulated keratinocytes.
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. 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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/15319796/ [2] https://pubmed.ncbi.nlm.nih.gov/27012991/

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