2. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  3. Histamine Receptor
  4. Levocetirizine

Levocetirizine  (Synonyms: (R)-Cetirizine)

Cat. No.: HY-B0814 Purity: 99.41%
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Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria.

For research use only. We do not sell to patients.

Levocetirizine Chemical Structure

Levocetirizine Chemical Structure

CAS No. : 130018-77-8

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5 mg USD 40 In-stock
10 mg USD 70 In-stock
25 mg USD 100 In-stock
50 mg USD 120 In-stock
100 mg USD 220 In-stock
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Based on 1 publication(s) in Google Scholar

Other Forms of Levocetirizine:

Levocetirizine Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Levocetirizine

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H1 Receptor H2 Receptor H3 Receptor H4 Receptor Histamine Receptor

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Levocetirizine ((R)-Cetirizine) is a third-generation peripheral H1-receptor antagonist. Levocetirizine is an antihistaminic agent which is the R-enantiomer of Cetirizine. Levocetirizine has a higher affinity for the histamine H1-receptor than (S)-Cetirizine and can effectively treat allergic rhinitis and chronic idiopathic urticaria[1].

IC50 & Target[1]

H1 Receptor

 

In Vivo

Levocetirizine (0.4 mg/kg; oral administration; male Sprague-Dawley rats) treatment shows that the Cmax, AUC0-t , AUC0-∞ and t1/2 are 0.34 μg/mL, 3.26 μg h/mL, 3.67 μg h/mL and 2.34 hours, respectively in Sprague-Dawley rats[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: 30 male Sprague-Dawley rats (8 weeks old; 200-250 g)[1]
Dosage: 0.4 mg/kg
Administration: Oral administration (Pharmacokinetic Analysis)
Result: The Cmax, AUC0-t , AUC0-∞ and t1/2 were 0.34 μg/mL, 3.26 μg h/mL, 3.67 μg h/mL and 2.34 hours, respectively.
Clinical Trial
Molecular Weight

388.89

Formula

C21H25ClN2O3
CAS No.
Appearance

Solid

Color

White to off-white

SMILES

O=C(O)COCCN1CCN([C@@H](C2=CC=C(Cl)C=C2)C3=CC=CC=C3)CC1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

4°C, sealed storage, away from moisture and light

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (257.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5714 mL 12.8571 mL 25.7142 mL
5 mM 0.5143 mL 2.5714 mL 5.1428 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 1

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
  • Protocol 2

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in Saline)

    Solubility: ≥ 2.5 mg/mL (6.43 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.5714 mL 12.8571 mL 25.7142 mL 64.2855 mL
5 mM 0.5143 mL 2.5714 mL 5.1428 mL 12.8571 mL
10 mM 0.2571 mL 1.2857 mL 2.5714 mL 6.4286 mL
15 mM 0.1714 mL 0.8571 mL 1.7143 mL 4.2857 mL
20 mM 0.1286 mL 0.6429 mL 1.2857 mL 3.2143 mL
25 mM 0.1029 mL 0.5143 mL 1.0286 mL 2.5714 mL
30 mM 0.0857 mL 0.4286 mL 0.8571 mL 2.1429 mL
40 mM 0.0643 mL 0.3214 mL 0.6429 mL 1.6071 mL
50 mM 0.0514 mL 0.2571 mL 0.5143 mL 1.2857 mL
60 mM 0.0429 mL 0.2143 mL 0.4286 mL 1.0714 mL
80 mM 0.0321 mL 0.1607 mL 0.3214 mL 0.8036 mL
100 mM 0.0257 mL 0.1286 mL 0.2571 mL 0.6429 mL
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Levocetirizine Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Levocetirizine130018-77-8(R)-CetirizineHistamine ReceptorInhibitorinhibitorinhibit

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