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Levocetirizine

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Catalog No. T1469Cas No. 130018-77-8
Alias Levocetirizine HCl

Levocetirizine is a Histamine-1 Receptor Antagonist. The mechanism of action of levocetirizine is as a Histamine H1 Receptor Antagonist.

Levocetirizine

Levocetirizine

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Purity: 99.94%
Catalog No. T1469Alias Levocetirizine HClCas No. 130018-77-8
Levocetirizine is a Histamine-1 Receptor Antagonist. The mechanism of action of levocetirizine is as a Histamine H1 Receptor Antagonist.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$32In StockIn Stock
10 mg$57In StockIn Stock
25 mg$82In StockIn Stock
50 mg$97In StockIn Stock
100 mg$182In StockIn Stock
200 mg$271-In Stock
1 mL x 10 mM (in DMSO)$35In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:99.94%
Color:White to Yellow
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Product Introduction

Levocetirizine AI Summary
Levocetirizine exhibits a range of significant bioactivities and pharmacokinetic properties. It acts as an inhibitor of multiple targets with various potencies: JMJD2A-Tudor Domain (89125.1 nM), Histone Lysine Methyltransferase G9a (39810.7 nM), BAZ2B (79432.8 nM), ERG Ets/DNA interaction (7943.3 nM), and USP1/UAF1 (89125.1 nM). Additionally, it functions as a ligand for beta-arrestin-biased ligands of the beta2-adrenergic receptor with a potency of 10000.0 nM, and it induces DNA re-replication in SW480 colon adenocarcinoma cells at a potency of 28183.8 nM. Pharmacokinetically, Levocetirizine displays high plasma protein binding of 85% in both human and guinea pig models and demonstrates a low ratio of unbound drug in the brain to plasma (Kp,uu,brain of 0.14) and a brain to plasma partition coefficient (Kp) of 0.22 in guinea pigs, indicating its limited brain penetration. The compound also exhibits antiviral activity against SARS-CoV-2 (USA-WA1/2020 strain) in HRCE cells, although the hit score (-0.05445) suggests potential off-disease activity. Moreover, Levocetirizine shows antimicrobial activities, specifically: - Antifungal activity against Candida albicans (0.53% inhibition) and Cryptococcus neoformans (0.71% inhibition) - Antibacterial activity against Escherichia coli (5.57% inhibition), Klebsiella pneumoniae (20.22% inhibition), Pseudomonas aeruginosa (6.8% inhibition), Acinetobacter baumannii (19.94% inhibition), and Staphylococcus aureus MRSA (11.65% inhibition) Lastly, it exhibits inhibitory activity toward human HDAC6, demonstrating slightly stronger inhibition in assays using custom peptide substrates compared to commercial ones..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
Levocetirizine is a Histamine-1 Receptor Antagonist. The mechanism of action of levocetirizine is as a Histamine H1 Receptor Antagonist.
SynonymsLevocetirizine HCl
Chemical Properties
Molecular Weight388.89
FormulaC21H25ClN2O3
Cas No.130018-77-8
Smiles[C@H](N1CCN(CCOCC(O)=O)CC1)(C2=CC=C(Cl)C=C2)C3=CC=CC=C3
Relative Density.1.237g/cm3
Storage & Solubility Information
Storagekeep away from direct sunlight,keep away from moisture,store under nitrogen | Pure form: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 22.5 mg/mL (57.86 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (5.14 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM2.5714 mL12.8571 mL25.7142 mL128.5711 mL
5 mM0.5143 mL2.5714 mL5.1428 mL25.7142 mL
10 mM0.2571 mL1.2857 mL2.5714 mL12.8571 mL
20 mM0.1286 mL0.6429 mL1.2857 mL6.4286 mL
50 mM0.0514 mL0.2571 mL0.5143 mL2.5714 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
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2 Enter the in vivo formulation:
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%
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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