Loratadine (Loratidine; SCH 29851)

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

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Size	Price	Stock
1g	$250	Check With Us
2g	$350	Check With Us
5g	$550	Check With Us

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Cat #: V1208 CAS #: 79794-75-5 Purity ≥ 98%

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 acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM. Loratadine lacks central nervous system depressing effects such as drowsiness. It has been shown to inhibit the release of leukotriene C4 and histamine from rodent mast cells and to inhibit allergic bronchospasm in guinea pigs. Loratadine is a selective inverse peripheral histamine H1-receptor agonist.

References: 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.

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Physicochemical and Storage Information
Protocol
Related Biological Data
Stock Solution Preparation
Quality Control Documentation

Molecular Weight (MW)	382.88
Molecular Formula	C22H23ClN2O2
CAS No.	79794-75-5
Storage	-20℃ for 3 years in powder formr
Storage	-80℃ for 2 years in solvent
Solubility In Vitro	DMSO: 17 mg/mL (44.4 mM)r
	Water: <1 mg/mLr
	Ethanol: 77 mg/mL (201.1 mM)
Solubility In Vivo	Chemical Name: ethyl 4-(8-chloro-5,6-dihydrobenzo[1,2]cyclohepta[2,4-b]pyridin-11-ylidene)piperidine-1-carboxylate 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 SMILES Code: CCOC(=O)N1CCC(=C2C3=C(CCC4=C2N=CC=C4)C=C(C=C3)Cl)CC1
SMILES Code	CCOC(=O)N1CCC(=C2C3=C(CCC4=C2N=CC=C4)C=C(C=C3)Cl)CC1
Synonyms	SCH29851; Loratadine; Claritin; Loratidine; Clarityn; Alavert; Loratadine; Sch 29851; Sch-29851; Sch29851

Protocol	In Vitro	In vitro activity: Loratadine is identified as a selective inhibitor of B(0)AT2 with an IC50 of 4 μM while being less active or inactive against several other members of the SLC6 family. Loratadine concentration-dependently inhibits the release of histamine and LTC4 when preincubating before Der p 1 antigen or anti-Fc epsilon RI challenge in human Fc epsilon RI+ cells. Loratadine (0.1 mM) also inhibits (10-40%) histamine, LTC4, and PGD2 release from purified HLMC (16-68%) activated by anti-Fc epsilon RI. Loratadine causes concentration-dependent inhibition (10-40%) of histamine, tryptase, LTC4, and PGD2 release from purified HSMC (24-72%) immunologically challenged with anti-Fc epsilon RI. Loratadine inhibits significantly IL-6 and IL-8 secretion induced by histamine with a more powerful efficiency of the active metabolite in human umbilical vein endothelial cells (HUVEC). Loratadine blocks hKv1.5 channels in a concentration-, voltage-, time- and use-dependent manner but only at concentrations much higher than therapeutic plasma levels in man in Ltk- cells transfected with the gene encoding hKv1.5 channels. Loratadine inhibits rhinovirus-induced ICAM-1 upregulation in both primary bronchial or transformed (A549) respiratory epithelial cells. Loratadine also inhibits ICAM-1 mRNA induction caused by rhinovirus infection in a dose-dependent manner, and they completely inhibits rhinovirus-induced ICAM-1 promoter activation. Cell Assay: Loratadine(SCH-29851) is a selective inverse peripheral histamine H1-receptor agonist with an IC50 of >32 μM. Loratadine is a non-sedative antihistamine that inhibits histamine-induced activities of IL-6 and IL-8 secretion in endothelial cells.

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

Preparing Stock Solutions

Solvent volume to be added	Mass (the weight of a compound)
Mother liquor concentration	1mg	5mg	10mg	20mg
1mM	2.6118 mL	13.0589 mL	26.1178 mL	52.2357 mL
5mM	0.5224 mL	2.6118 mL	5.2236 mL	10.4471 mL
10mM	0.2612 mL	1.3059 mL	2.6118 mL	5.2236 mL
20mM	0.1306 mL	0.6529 mL	1.3059 mL	2.6118 mL

Quality Control Documentation	Select Batch Purity ≥ 98% COA MSDS NMR HPLC

The molarity calculator equation

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

Mass

Concentration

Volume

Molecular Weight*

The dilution calculator equation

Concentration_(start) × Volume_(start) = Concentration_(final) × Volume_(final)

This equation is commonly abbreviated as: C₁ V₁ = C₂ V₂

Concentration_(start)

Volume_(start)

Concentration_(final)

Volume_(final)

Step One: Enter information below

Dosage mg/kg Average weight of animals g Dosing volume per animal µL Number of animals

Step Two: Enter the in vivo formulation

%DMSO + % + %Tween 80 + %ddH₂O

Calculation Results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in µL DMSO(Master liquid 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 master liquid, next add µL PEG300, mix and clarify, next add µL 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.