Cat. No.: HY-17043

Loratadine

(Synonyms: Loratidine; SCH 29851)

11 Cited Publications

Customer Review

Based on 11 publication(s) in Google Scholar

Loratadine (SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine has anti-dengue-virus (DENV) activity. Loratadine can inhibit immunologic release of inflammatory mediators.

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

Purity: 99.98%
CAS No.: 79794-75-5
Formula: C₂₂H₂₃ClN₂O₂
Molecular Weight:382.88

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Loratadine Chemical Structure

CAS No.: 79794-75-5

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (11)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

H₁ Receptor

All Histamine Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
Caco-2	CC₅₀	28.33 μM Compound: LORATADINE	Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay	10.21203/rs.3.rs-23951/v1
Caco-2	IC₅₀	15.13 μM Compound: LORATADINE	Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging	10.21203/rs.3.rs-23951/v1
CHO	IC₅₀	11.4 μM Compound: loratadine	Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits	[PMID: 23812503]
HEK293	IC₅₀	4 μM Compound: 1	Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay Inhibition of eGFP-tagged human B0AT2 expressed in HEK293 cells measured within 10 mins by [3H]proline uptake assay	[PMID: 25318072]
HEK293	IC₅₀	63.4 μM Compound: 24	Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay Inhibition of human TASK3 expressed in HEK293 cells by Ti+ flux assay	[PMID: 31260312]
HepG2	EC₅₀	10 μM Compound: Loratadine	Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells after 24 hrs by luciferase reporter gene based luminescent analysis	[PMID: 20966043]
HepG2	EC₅₀	12.6 μM Compound: Loratadine	Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis Activation of human PXR expressed in human HepG2 (DPX-2) cells assessed as induction of CYP3A4 after 24 hrs by luminescent analysis	[PMID: 20966043]
HepG2	EC₅₀	3 μM Compound: 8	Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay Agonist activity at PXR (unknown origin) expressed in human HepG2 cells assessed as induction of CYP3A4 transactivation after 16 hrs by luciferase reporter gene assay	[PMID: 23688559]
HT-29	IC₅₀	6.2 μM Compound: 4	Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 144 hrs by crystal violet staining method Antiproliferative activity against human HT-29 cells assessed as growth inhibition after 144 hrs by crystal violet staining method	[PMID: 22450132]
HT-29	IC₅₀	6.2 μM Compound: Loratadine	Cytotoxicity against human HT-29 cells after 72 hrs by crystal violet staining Cytotoxicity against human HT-29 cells after 72 hrs by crystal violet staining	[PMID: 22959205]
MCF7	IC₅₀	7.5 μM Compound: 4	Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 144 hrs by crystal violet staining method Antiproliferative activity against human MCF7 cells assessed as growth inhibition after 144 hrs by crystal violet staining method	[PMID: 22450132]
MCF7	IC₅₀	7.5 μM Compound: Loratadine	Cytotoxicity against human MCF7 cells after 72 hrs by crystal violet staining Cytotoxicity against human MCF7 cells after 72 hrs by crystal violet staining	[PMID: 22959205]
MDA-MB-231	IC₅₀	8.4 μM Compound: 4	Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 144 hrs by crystal violet staining method Antiproliferative activity against human MDA-MB-231 cells assessed as growth inhibition after 144 hrs by crystal violet staining method	[PMID: 22450132]
MDA-MB-231	IC₅₀	8.4 μM Compound: Loratadine	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by crystal violet staining Cytotoxicity against human MDA-MB-231 cells after 72 hrs by crystal violet staining	[PMID: 22959205]

In Vitro

Loratadine is an antihistamine that inhibits histamine-induced activities of IL-6 and IL-8 secretion in endothelial cells.

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 79794-75-5
Appearance Solid
Molecular Weight 382.88
Formula C₂₂H₂₃ClN₂O₂
Color White to off-white
SMILES

O=C(N1CC/C(CC1)=C2C3=CC=C(Cl)C=C3CCC4=CC=CN=C4\2)OCC
Synonyms

Loratidine; SCH 29851
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

Publications (11)

All In Vivo Efficacy StudyBio/Physico-chemical AssayCell Proliferation/Viability AssayFlow Cytometry

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Journal Impact Factor

Front Pharmacol

Metabolomics combined with molecular docking and dynamics simulation to investigate the mechanism of action of Fibraurea recisa Pierre in the treatment of chronic urticaria. [Abstract]

2025 May 21:16:1571819. PMID: 40469983
Int Immunopharmacol

Melastoma dodecandrum polysaccharide alleviates allergic rhinitis in mice through modulating NLRP3 and IL-17 axis. [Abstract]

2025 Jun 8:161:115054. PMID: 40489908
Eur J Pharmacol

Xanthotoxol relieves itch in mice via suppressing spinal GRP/GRPR signaling. [Abstract]

2023 Dec 5:960:176147. PMID: 37871763

Loratadine purchased from MedChemExpress. Usage Cited in: Eur J Pharmacol. 2023 Dec 5:960:176147. [Abstract]

Loratadine (10 mg/kg; i.p.; 30 min) suppressed itch in compound 48/80-treated mice but not in CQ-treated mice.
Neuropharmacology

Imperatorin activates TRPV1/GRPR pathway to induce scratching behaviors in mice. [Abstract]

2025 Nov 1:278:110593. PMID: 40683349
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
Pharm Res

Investigation of the Binding Characteristics of Agonists and Various Antagonists Targeting Histamine 1 Receptor. [Abstract]

2025 Aug;42(8):1315-1329. PMID: 40760405
iScience

Loratadine inhibits Staphylococcus aureus virulence and biofilm formation. [Abstract]

2022 Jan 5;25(2):103731. PMID: 35098100
Sci Rep

Cannabis constituents interact at the drug efflux pump BCRP to markedly increase plasma cannabidiolic acid concentrations. [Abstract]

2021 Jul 22;11(1):14948. PMID: 34294753

Loratadine purchased from MedChemExpress. Usage Cited in: Sci Rep. 2021 Jul 22;11(1):14948. [Abstract]

Concentration-time curves for prazosin in the presence of Loratadine (10 μM; 60-240 min) in the basolateral to apical (B > A) and apical to basolateral (A > B) directions in MDCKs expressing BCRP.
ACS Infect Dis

Loratadine Derivative Lo-7: A Weapon against Drug-Resistant Enterococcus and Streptococcal Infections. [Abstract]

2024 Aug 9;10(8):2961-2977. PMID: 39066703

Loratadine purchased from MedChemExpress. Usage Cited in: ACS Infect Dis. 2024 Aug 9;10(8):2961-2977. [Abstract]

Loratadine (25−100 μM, 24 h) effectively impeded the formation of E. faecalis biofilms.

Loratadine purchased from MedChemExpress. Usage Cited in: ACS Infect Dis. 2024 Aug 9;10(8):2961-2977. [Abstract]

Loratadine (50 μM, 24 h) hindered the biofilm formation of 8 out of 11 clinical E. faecalis isolates.

Loratadine purchased from MedChemExpress. Usage Cited in: ACS Infect Dis. 2024 Aug 9;10(8):2961-2977. [Abstract]

Loratadine (50 μM, 24 h) exhibited a significant inhibitory impact on the biofilm formation of the E. faecalis FB-1 strain.
J Clin Psychopharmacol

A Potential Drug-Gene-Drug Interaction Between Cannabidiol, CYP2D6*4, and Fluoxetine: A Case Report. [Abstract]

2022 Jul-Aug;42(4):422-424. PMID: 35652796
Biochem Biophys Res Commun

Dual-cardiotoxicity evaluation of torsadogenic risk drugs using human iPSC-derived cardiomyocytes. [Abstract]

2025 Oct 30:786:152756. PMID: 41043280

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (130.59 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6118 mL

13.0589 mL

26.1178 mL

5 mM

0.5224 mL

2.6118 mL

5.2236 mL

10 mM

0.2612 mL

1.3059 mL

2.6118 mL

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

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In Vivo:

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

Stock Solution Working Solution

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 (6.53 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.

Protocol 2

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

Solubility: ≥ 2.5 mg/mL (6.53 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.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.53 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

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).

Working solution concentration: 0.22 mg/mL

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (279 KB)
SDS (458 KB)
- English - EN (458 KB)
- Français - FR (458 KB)
- Deutsch - DE (458 KB)
- Norwegian - NO (458 KB)
- Español - ES (458 KB)
- Swedish - SV (458 KB)
- Italian - IT (458 KB)
- Portuguese - PT (458 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Kay GG, Harris AG. Loratadine: a non-sedating antihistamine. Review of its effects on cognition, psychomotor performance, mood and sedation. Clin Exp Allergy. 1999 Jul;29 Suppl 3:147-50. [Content Brief]

[2]. Menardo JL, Horak F, Danzig MR, Czarlewski W. A review of loratadine in the treatment of patients with allergic bronchial asthma. Clin Ther. 1997 Nov-Dec;19(6):1278-93; discussion 1523-4. [Content Brief]

[3]. Monroe EW. Loratadine in the treatment of urticaria. Clin Ther. 1997 Mar-Apr;19(2):232-42. [Content Brief]

[4]. Haria M, Fitton A, Peters DH. Loratadine. A reappraisal of its pharmacological properties and therapeutic use in allergic disorders. Drugs. 1994 Oct;48(4):617-37. [Content Brief]

[5]. Roman IJ, Danzig MR. Loratadine. A review of recent findings in pharmacology, pharmacokinetics, efficacy, and safety, with a look at its use in combination with pseudoephedrine. Clin Rev Allergy. 1993 Spring;11(1):89-110. [Content Brief]

[6]. Shahen M, et al. Dengue virus causes changes of MicroRNA-genes regulatory network revealing potential targets for antiviral drugs. BMC Syst Biol. 2018 Jan 4;12(1):2. [Content Brief]

[7]. Kleine-Tebbe J, et al. Inhibition of IgE- and non-IgE-mediated histamine release from human basophil leukocytes in vitro by a histamine H1-antagonist, desethoxycarbonyl-loratadine. J Allergy Clin Immunol. 1994;93(2):494-500. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6118 mL	13.0589 mL	26.1178 mL	65.2946 mL
	5 mM	0.5224 mL	2.6118 mL	5.2236 mL	13.0589 mL
	10 mM	0.2612 mL	1.3059 mL	2.6118 mL	6.5295 mL
	15 mM	0.1741 mL	0.8706 mL	1.7412 mL	4.3530 mL
	20 mM	0.1306 mL	0.6529 mL	1.3059 mL	3.2647 mL
	25 mM	0.1045 mL	0.5224 mL	1.0447 mL	2.6118 mL
	30 mM	0.0871 mL	0.4353 mL	0.8706 mL	2.1765 mL
	40 mM	0.0653 mL	0.3265 mL	0.6529 mL	1.6324 mL
	50 mM	0.0522 mL	0.2612 mL	0.5224 mL	1.3059 mL
	60 mM	0.0435 mL	0.2176 mL	0.4353 mL	1.0882 mL
	80 mM	0.0326 mL	0.1632 mL	0.3265 mL	0.8162 mL
	100 mM	0.0261 mL	0.1306 mL	0.2612 mL	0.6529 mL

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Loratadine

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Publications Citing Use of MedChemExpress (MCE) Loratadine

All Histamine Receptor Isoforms

Biological Activity

Chemical Information

Publications (11)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Loratadine Related Classifications

Cat. No.: HY-17043