Loratadine (Synonyms: Loratidine; SCH 29851)

Name: Loratadine
Brand: MedChemExpress
SKU: HY-17043
Rating: 5.0 (11 reviews)

Cat. No.: HY-17043 Purity: 99.98%: Data Sheet
COA

SDS
Handling Instructions
FAQs
Technical Support

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.

CAS No. : 79794-75-5

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
50 mg	In-stock	Estimated Time of Arrival: December 31
100 mg	In-stock	Estimated Time of Arrival: December 31
500 mg	In-stock	Estimated Time of Arrival: December 31
1 g	Get quote
5 g	Get quote

or Bulk Inquiry

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 11 publication(s) in Google Scholar

Other Forms of Loratadine:

11 Publications Citing Use of MCE Loratadine

In Vivo Efficacy Study

Bio/Physico-chemical Assay

Cell Proliferation/Viability Assay

Flow Cytometry

: 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.

: 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.

: 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.

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histamine Receptor Isoform Specific Products:

View All Isoforms

H₁ Receptor H₂ Receptor H₃ Receptor H₄ Receptor Histamine Receptor

Biological Activity
Purity & Documentation
References
Customer Review

Description

IC₅₀ & Target

H₁ Receptor

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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
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]
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]
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]
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

Molecular Weight

382.88

Formula

C₂₂H₂₃ClN₂O₂

CAS No.

79794-75-5

Appearance

Solid

Color

White to off-white

SMILES

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

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

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)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

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, 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
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

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 (6.53 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.
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 (6.53 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.
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.
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

mg/kg

Animal weight
(per animal)

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).

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

Purity: 99.98%

Select Batch:

Data Sheet (279 KB) SDS (458 KB)

COA (255 KB) HNMR (128 KB) RP-HPLC (246 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]

Complete Stock Solution Preparation Table

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

Loratadine 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:

Loratadine79794-75-5Loratidine SCH 29851SCH29851SCH 29851SCH-29851Dengue VirusFlavivirusHistamine ReceptorDENVInhibitorinhibitorinhibit

Your Recently Viewed Products:

Product Name

Requested Quantity *

Applicant Name *

Salutation

Email Address *

Phone Number *

Department

Organization Name *

City

State

Country or Region *

Remarks

Product Name

Lot #

Applicant Name *

Email Address *

Phone Number

Department *

Organization Name *

Country or Region *

Remarks

Name
Email *

	Sorry, but the email address you supplied was invalid.

Loratadine (Synonyms: Loratidine; SCH 29851)

Customer Review

Other Forms of Loratadine:

Loratadine Related Antibodies

11 Publications Citing Use of MCE Loratadine

Featured Recommendations

•Related Screening Libraries:

•Related Small Molecules:

•Related Proteins:

View All Histamine Receptor Isoform Specific Products:

Biological Activity

Purity & Documentation

References

Customer Review

Loratadine Related Antibodies

Molarity Calculator

Dilution Calculator

Complete Stock Solution Preparation Table

Loratadine Related Classifications

Keywords:

Your Recently Viewed Products:

Customer Review

Request for HNMR Report

SAFETY DATA SHEET (SDS)

Request for HNMR Report