Loratadine (Loratidine; SCH 29851)

Alias: SCH29851; Loratadine; Claritin; Loratidine; Clarityn; Alavert; Loratadine; Sch 29851; Sch-29851; Sch29851

Cat No.:V1208 Purity: ≥98%

COA Product Data Instructions for use SDS

Loratadine (Loratidine; SCH 29851) Chemical Structure CAS No.: 79794-75-5
Product category: Histamine Receptor

This product is for research use only, not for human use. We do not sell to patients.

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Other Forms of Loratadine (Loratidine; SCH 29851):

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Top Publications Citing lnvivochem Products

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J Am Chem Soc 2022,144:21831-21836.

Cell 2020,183:1202-1218.e25.

Science Adv 2022:8,eabm9427.

Nature 2021,597(7874):119-125.

Cell 2020,183:1202-1218.e25.

PNAS Nexus 2022,1(3):pgac063.

ACS Nano 2023,17(10):9110-9125.

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Purity & Quality Control Documentation

Current batch：

Purity: ≥98%

COA

MSDS

NMR

Instructions

Product Description
Bioactivity & Protocols
Physicochemical Properties
Solubility Data
Calculators
Clinical Trial Information
Biological Data

Product Description

Loratadine (formerly SCH29851; SCH-29851; Claritin; Loratidine; Clarityn; Alavert) is a potent and 2nd-generation histamine H1 receptor antagonist which has been approved for the treatment of allergies such as allergic rhinitis and urticaria. It also functions as a selective inhibitor of B(0)AT2 with IC50 of 4 μM. Loratadine doesn't have any effects that depress the central nervous system, like sleepiness. It has been demonstrated to suppress histamine and leukotriene C4 release from rodent mast cells as well as to suppress allergic bronchospasm in guinea pigs. Loratadine is an inverse peripheral histamine H1-receptor agonist that is selective.

Biological Activity I Assay Protocols (From Reference)

Targets

H1 receptor; B(0)AT2 ( IC50 = 4 μM )

ln Vitro

In vitro activity: Loratadine has been found to be a less active or inactive inhibitor of various other SLC6 family members, but it is a selective inhibitor of B(0)AT2 with an IC50 of 4 μM.[1] Loratadine suppresses the release of histamine and LTC4 in human Fc epsilon RI+ cells in a concentration-dependent manner when preincubated prior to Der p 1 antigen or anti-Fc epsilon RI challenge. Loratadine (0.1 mM) also prevents the release of PGD2, LTC4, and histamine (10–40%) from purified HLMC (16–68%) that have been activated by anti-Fc epsilon RI. In purified HSMC (24–72%) immunologically challenged with anti-Fc epsilon RI, loratadine causes concentration-dependent inhibition (10–40%) of histamine, tryptase, LTC4, and PGD2 release.[2] In human umbilical vein endothelial cells (HUVEC), loratadine significantly reduces the secretion of IL-6 and IL-8 that is triggered by histamine, with a more potent efficiency of the active metabolite.[3] Loratadine inhibits human hKv1.5 channels in Ltk-cells transfected with the hKv1.5 channel gene in a concentration-, voltage-, time-, and use-dependent manner, but only at concentrations significantly higher than therapeutic plasma levels.[4] Loratadine prevents the upregulation of ICAM-1 caused by rhinoviruses in respiratory epithelial cells, whether they are primary bronchial or transformed (A549). Additionally, loratadine completely blocks the activation of the ICAM-1 promoter induced by rhinovirus infection and inhibits the dose-dependent induction of ICAM-1 mRNA.[5]

ln Vivo

Animal Protocol

References

[1]. J Med Chem . 2014 Nov 26;57(22):9473-9.

[2]. Clin Exp Allergy . 1997 May;27(5):559-67.

[3]. Clin Exp Allergy . 1997 Oct;27(10):1167-74.

[4]. Cardiovasc Res . 1997 Aug;35(2):341-50.

[5]. J Allergy Clin Immunol . 2001 Aug;108(2):221-8.

These protocols are for reference only. InvivoChem does not independently validate these methods.

Physicochemical Properties

Molecular Formula

C22H23CLN2O2

Molecular Weight

382.88

Exact Mass

382.14

Elemental Analysis

C, 69.01; H, 6.05; Cl, 9.26; N, 7.32; O, 8.36

CAS #

79794-75-5

Related CAS #

Loratadine-d4; 381727-27-1; Loratadine-d5; 1398065-63-8

Appearance

Solid powder

SMILES

CCOC(=O)N1CCC(=C2C3=C(CCC4=C2N=CC=C4)C=C(C=C3)Cl)CC1

InChi Key

JCCNYMKQOSZNPW-UHFFFAOYSA-N

InChi Code

InChI=1S/C22H23ClN2O2/c1-2-27-22(26)25-12-9-15(10-13-25)20-19-8-7-18(23)14-17(19)6-5-16-4-3-11-24-21(16)20/h3-4,7-8,11,14H,2,5-6,9-10,12-13H2,1H3

Chemical Name

ethyl 4-(13-chloro-4-azatricyclo[9.4.0.03,8]pentadeca-1(11),3(8),4,6,12,14-hexaen-2-ylidene)piperidine-1-carboxylate

Synonyms

SCH29851; Loratadine; Claritin; Loratidine; Clarityn; Alavert; Loratadine; Sch 29851; Sch-29851; Sch29851

HS Tariff Code

2934.99.9001

Storage

Powder -20°C 3 years

4°C 2 years

In solvent -80°C 6 months

-20°C 1 month

Shipping Condition

Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Solubility Data

Solubility (In Vitro)

DMSO: 17~50 mg/mL (44.4~130.6 mM)

Water: <1 mg/mL

Ethanol: ~77 mg/mL (~201.1 mM)

Solubility (In Vivo)

Solubility in Formulation 1: ≥ 2.5 mg/mL (6.53 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.5 mg/mL (6.53 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.5 mg/mL (6.53 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

Solubility in Formulation 4: 5%DMSO + Corn oil: 4.0mg/ml (10.45mM)

(Please use freshly prepared in vivo formulations for optimal results.)

Preparing Stock Solutions		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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

Mass

Concentration

Volume

Molecular Weight*

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Molarity Calculator allows you to calculate the mass, volume, and/or concentration required for a solution, as detailed below:

Calculate the Mass of a compound required to prepare a solution of known volume and concentration
Calculate the Volume of solution required to dissolve a compound of known mass to a desired concentration
Calculate the Concentration of a solution resulting from a known mass of compound in a specific volume

See Example

An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?

Enter 350.26 in the Molecular Weight (MW) box
Enter 10 in the Concentration box and choose the correct unit (mM)
Enter 5 in the Volume box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Concentration (Start)

Volume (Start)

Concentration (End)

Volume (End)

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Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:

Enter 10 into the Concentration (Start) box and choose the correct unit (mM)
Enter 25 into the Concentration (End) box and select the correct unit (mM)
Enter 25 into the Volume (End) box and choose the correct unit (mL)
Click the “Calculate” button
The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box

Molecular formula

Total molecular weight

g/mol

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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4 c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:

To calculate molar mass of a chemical compound, please enter the chemical/molecular formula and click the “Calculate’ button.

Definitions of molecular mass, molecular weight, molar mass and molar weight:

Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

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Reconstitution Calculator allows you to calculate the volume of solvent required to reconstitute your vial.

Enter the mass of the reagent and the desired reconstitution concentration as well as the correct units
Click the “Calculate” button
The answer appears in the Volume (to add to vial) box

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal to make 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 in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)

% DMSO

% Tween 80

% ddH₂O

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Calculation results

Working concentration： mg/mL；

Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O，mix and clarify.

Note： (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.

Clinical Trial Information

NCT Number	Recruitment	interventions	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT05421416	Not yet recruiting	Drug: Loratadine Drug: Placebo	Stem Cell Transplant Complications	AHS Cancer Control Alberta	November 1, 2023	Phase 2
NCT05243706	Not yet recruiting	Drug: Loratadine Drug: Diosmin/ Hesperidin	Vinca Alkaloid Adverse Reaction	Ain Shams University	March 1, 2022	Phase 3
NCT04211259	Recruiting	Drug: Loratadine Other: Placebo	Plasma Cell Myeloma	Rutgers, The State University of New Jersey	April 18, 2022	Early Phase 1
NCT06217367	Recruiting	Drug: 10 mg Loratadine Drug: 5 mg Desloratadine	Heat Illness Allergic Rhinitis Heat Injury	Lakehead University	December 5, 2023	Phase 4
NCT02513290	Completed	Drug: Bilastine Drug: Loratadine	Allergic Rhinitis	Universidade do Sul de Santa Catarina	August 2013	Phase 4

Biological Data

Effects of loratadine on hKv1.5 channels expressed in a mouse L-cell. Cardiovasc Res . 1997 Aug;35(2):341-50.
Concentration dependence of loratadine-induced block of hKv1.5. Cardiovasc Res . 1997 Aug;35(2):341-50.
Effect of 1 μM loratadine on the steady-state current–voltage (I–V) relationships (500 ms isochronal). Cardiovasc Res . 1997 Aug;35(2):341-50.