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Loratadine

Catalog No. T1097   CAS 79794-75-5
Synonyms: SCH 29851, Loratidine

Loratadine (SCH 29851) is a second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.

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Loratadine Chemical Structure
Loratadine, CAS 79794-75-5
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Purity: 99.75%
Purity: 99.49%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Loratadine (SCH 29851) is a second-generation histamine H1 receptor antagonist used in the treatment of allergic rhinitis and urticaria. Unlike most classical antihistamines (HISTAMINE H1 ANTAGONISTS) it lacks central nervous system depressing effects such as drowsiness.
Targets&IC50 B(0)AT2:4 μM
In vivo Loratadine blocks Kv1.5 channels in a concentration-, voltage-, time-, and use-dependent manner when expressed in human Ltk-cells transfected with the hKv1.5 channel gene at concentrations exceeding therapeutic plasma levels. It also inhibits rhinovirus-induced upregulation of ICAM-1 in main bronchial or transformed respiratory epithelial cells. Identified as a selective inhibitor of B(0)AT 2 with an IC50 of 4 μM, loratadine exhibits low or no activity against several other members of the SLC6 family. Pre-incubation with loratadine concentration-dependently suppresses the release of histamine and LTC4 in human FcεRI+ cells upon challenge with Der p1 antigen or anti-FcεRI. In human umbilical vein endothelial cells, loratadine significantly inhibits histamine-induced secretion of IL-6 and IL-8, with its active metabolites showing even stronger effects. Additionally, loratadine in a dose-dependent manner inhibits the mRNA of ICAM-1 induced by rhinovirus infection and completely suppresses the activation of the rhinovirus-induced ICAM-1 promoter.
Synonyms SCH 29851, Loratidine
Molecular Weight 382.88
Formula C22H23ClN2O2
CAS No. 79794-75-5

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

Ethanol: 77 mg/mL (201.1 mM)

DMSO: 17 mg/mL (44.4 mM)

TargetMolReferences and Literature

1. Cuboni S, et al. J Med Chem, 2014, 57(22), 9473-9479. 2. Genovese A, et al. Clin Exp Allergy, 1997, 27(5), 559-567. 3. Molet S, et al. Clin Exp Allergy, 1997, 27(10), 1167-1174. 4. Delpón E, et al. Cardiovasc Res. 1997 Aug;35(2):341-50. 5. Papi A, et al. J Allergy Clin Immunol, 2001, 108(2), 221-228.

Related compound libraries

This product is contained In the following compound libraries:
GPCR Compound Library Inhibitor Library Anti-Cancer Approved Drug Library Anti-Cancer Clinical Compound Library Drug Repurposing Compound Library Anti-Cancer Drug Library NO PAINS Compound Library Bioactive Compounds Library Max Clinical Compound Library Pediatric Drug Library

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Keywords

Loratadine 79794-75-5 GPCR/G Protein Immunology/Inflammation Microbiology/Virology Neuroscience Influenza Virus Histamine Receptor SCH-29851 inhibit SCH29851 SCH 29851 Inhibitor Loratidine inhibitor

 

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