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[CAS NO. 79794-75-5] Loratadine

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Catalog:	HY-17043
Brand:	MCE
CAS:	79794-75-5

Overview

MDL	MFCD00672869
Molecular Weight	382.88
Molecular Formula	C22H23ClN2O2
SMILES	O=C(N1CC/C(CC1)=C2C3=CC=C(Cl)C=C3CCC4=CC=CN=C4\2)OCC

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

3 Publications Citing Use of MCE

[1]iScience. 5 January 2022, 103731.
[2]Sci Rep. 2021 Jul 22;11(1):14948.
[3]J Clin Psychopharmacol. 2022 Jun 2.

Summary

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.

IC50 & Target

H ₁ Receptor

In Vitro

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

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

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase
NCT02495077	National Institute of Allergy and Infectious Diseases (NIAID)\|Clinical Trials in Organ Transplantation\|Rho Federal Systems Division, Inc.	Kidney Transplant	November 2, 2015	Phase 2
NCT02007434	Kythera Biopharmaceuticals	Moderate or Severe Submental Fullness	December 2013	Phase 3
NCT00963599	Organon and Co	Seasonal Allergic Rhinitis	September 1999	Phase 3
NCT00721331	Zalicus	Atopic Dermatitis	July 2008	Phase 1
NCT03004131	MEDA Pharma GmbH & Co. KG\|Viatris Inc.	Seasonal Allergic Rhinitis	January 7, 2017	Phase 4
NCT01311336	University of Vermont\|Cancer and Leukemia Group B	Pegfilgrastim-induced Back and Leg Pain	May 2011	Phase 2
NCT00837915	Ranbaxy Laboratories Limited\|Ranbaxy Inc.	Healthy	June 2002	Not Applicable
NCT03517930	Bayer	Clinical Pharmacology	April 17, 2018	Phase 1
NCT00776282	Ranbaxy Laboratories Limited\|Ranbaxy Inc.	Healthy	July 2006	Not Applicable
NCT01712009	Amgen	Bone Pain in Stage I - III Breast Cancer	November 1, 2012	Phase 2
NCT02392039	M.D. Anderson Cancer Center\|Amgen	Lymphoma	December 14, 2015	Early Phase 1
NCT01700192	ALK-Abelló A+S\|Merck Sharp & Dohme LLC	Rhinitis, Allergic, Perennial\|Rhinitis, Allergic, Nonseasonal	January 2013	Phase 3
NCT02932774	Johnson & Johnson Consumer and Personal Products Worldwide\|Pfizer	Allergic Rhinitis\|Hay Fever\|SAR\|Rhinitis, Allergic, Seasonal	March 2001	Phase 4
NCT03640273	Thammasat University	Allergic Rhinitis\|Adverse Drug Event\|Quality of Life	November 23, 2017	Phase 2
NCT04211259	Rutgers, The State University of New Jersey\|National Cancer Institute (NCI)	Plasma Cell Myeloma	April 18, 2022	Early Phase 1
NCT03883386	University of Michigan	Bone Pain	June 24, 2019	Phase 2
NCT02513290	Universidade do Sul de Santa Catarina	Allergic Rhinitis	August 2013	Phase 4
NCT02478398	Merck Sharp & Dohme LLC	Rhinitis, Allergic, Seasonal	July 20, 2015	Phase 3
NCT03443843	Bayer	Rhinitis, Allergic	February 21, 2018	Phase 4
NCT03855228	Organon and Co	Rhinitis, Allergic	March 1, 1995	Phase 3
NCT00730912	Merck Sharp & Dohme LLC	Perennial Allergic Rhinitis	June 2008	Phase 4
NCT00979901	Organon and Co	Seasonal Allergic Rhinitis	March 2000	Phase 3
NCT00963573	Merck Sharp & Dohme LLC	Rhinitis	September 2003	Phase 4
NCT02576808	Thai Traditional Medical Knowledge Fund\|Thammasat University	Rhinitis,Allergic	October 2015	Phase 2
NCT01413958	Bayer	Seasonal Allergic Rhinitis	August 2011	Phase 3
NCT02305979	Wake Forest University Health Sciences	Leukemia\|Lymphoma	December 2014
NCT00972738	Organon and Co	Seasonal Allergic Rhinitis	April 2001	Phase 3
NCT05421416	AHS Cancer Control Alberta	Stem Cell Transplant Complications	November 1, 2022	Phase 2
NCT05265910	Andover Research Eye Institute	Allergic Conjunctivitis	December 14, 2021	Phase 4
NCT00481676	Novartis	Chronic Urticaria	May 2007	Phase 2
NCT02593747	Bayer	Histamine H1 Antagonists, Non-Sedating	December 2015	Phase 1
NCT02653339	Peking Union Medical College Hospital	Rhinitis, Allergic, Perennial	June 2016	Not Applicable
NCT01055756	Azidus Brasil	Allergic Rhinitis	January 2010	Phase 3
NCT01330017	Bayer	Rhinitis\|Seasonal Rhinitis	March 2011	Phase 2
NCT01469234	Bayer	Rhinitis	October 2011	Phase 4
NCT05190627	Institut d´Investigació Biomèdica de Bellvitge	Lymphangioleiomyomatosis	November 1, 2021	Phase 2
NCT02339714	Zhao Hong\|China Academy of Chinese Medical Sciences\|Beijing Municipal Science & Technology Commission	Rhinitis, Allergic, Perennial	March 2015	Phase 2
NCT03372473	Innovacion y Desarrollo de Estrategias en Salud\|National Institute of Pediatrics, Mexico\|Laboratorios Senosiain, S.A. de C.V.	Asthma in Children	January 10, 2016	Phase 3
NCT02583594	Genzyme, a Sanofi Company\|Sanofi	Progressive Multiple Sclerosis	December 6, 2015	Phase 1
NCT00562159	ALK-Abelló A+S	Rhinoconjunctivitis\|Rhinitis\|Conjunctivitis\|Allergy	November 2007	Phase 3
NCT03151720	Xian-Janssen Pharmaceutical Ltd.	Healthy	June 1, 2017	Phase 1
NCT00960141	Organon and Co	Seasonal Allergic Rhinitis	August 2000	Phase 3
NCT05243706	Ain Shams University	Vinca Alkaloid Adverse Reaction	March 1, 2022	Phase 3
NCT03517943	Bayer	Clinical Pharmacology	April 24, 2018	Phase 1
NCT00963469	Organon and Co	Seasonal Allergic Rhinitis	August 2001	Phase 3
NCT00762983	Merck Sharp & Dohme LLC	Rhinitis, Allergic, Seasonal\|Rhinitis, Allergic, Perennial\|Urticaria\|Pruritus	March 2008
NCT03196531	Xian-Janssen Pharmaceutical Ltd.	Healthy	November 7, 2017	Phase 1
NCT05043350	Ain Shams University\|Nasr City Insurance Hospital	Covid19	September 13, 2021	Phase 2\|Phase 3
NCT04162795	Bayer	Allergic Rhinitis	November 12, 2019	Phase 4
NCT00561717	Bayer\|Queen´s University	Seasonal Allergic Rhinitis	October 2007	Phase 4
NCT00550550	ALK-Abelló A+S	Rhinoconjunctivitis\|Rhinitis\|Conjunctivitis\|Allergy	November 2007	Phase 3
NCT04248712	Mayo Clinic	Eosinophilic Esophagitis	July 10, 2020	Phase 2
NCT03376594	Thammasat University	Allergic Rhinitis	July 30, 2017	Phase 2
NCT01390441	Merck Sharp & Dohme LLC	Rheumatoid Arthritis	July 2011	Phase 1
NCT00946608	Sandoz	Allergy	June 2005	Phase 1
NCT00776217	Ranbaxy Laboratories Limited\|Ranbaxy Inc.	Healthy	June 2006	Not Applicable

Appearance

Solid

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL ( 130.59 mM ; Need ultrasonic)

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

* Please refer to the solubility information to select the appropriate solvent.

In Vivo:

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
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
3.

Add each solvent one by one: 10% DMSO >> 90% corn oil

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

* All of the co-solvents are available by MCE.

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

Synonyms

1-Piperidinecarboxylic acid, 4-(8-chloro-5,6-dihydro-11H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-ylidene)-, ethyl ester

11H-Benzo[5,6]cyclohepta[1,2-b]pyridine, 1-piperidinecarboxylic acid deriv.

Sch 29851

Loratadine

Loratidine

Klaritin

Claritin

Bonalerg

Civeran

Anhissen

Claritine

Clarityn

Claratyne

Cronopen

Fristamin

Histaloran

Lertamine

Lisino

Loracert

Clarityne

Loranox

Lorastine

Loratyne

Lorfast

Lowadina

Optimin

Polaratyne

Pylor

Restamine

Sensibit

Sohotin

Tadine

Velodan

Zeos

Loradex

Alavert

Flonidan

Klarifer

Clarotadin

Erolin

Lomilan

Symphoral

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