Catalog No.S1358 Synonyms: SCH29851
Molecular Weight(MW): 382.88
Loratadine is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
Purity & Quality Control
Choose Selective Histamine Receptor Inhibitors
|Description||Loratadine is a histamine H1 receptor antagonist, used to treat allergies. Also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.|
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. 
-  Cuboni S, et al. J Med Chem, 2014, 57(22), 9473-9479.
-  Genovese A, et al. Clin Exp Allergy, 1997, 27(5), 559-567.
-  Molet S, et al. Clin Exp Allergy, 1997, 27(10), 1167-1174.
|In vitro||Ethanol||76 mg/mL (198.49 mM)|
|DMSO||17 mg/mL (44.4 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT03196531||Completed||Healthy||Xian-Janssen Pharmaceutical Ltd.||November 7 2017||Phase 1|
|NCT00751218||Completed||Urticaria||Merck Sharp & Dohme Corp.||May 6 2004||Phase 4|
|NCT01673620||Completed||Allergic Rhinitis||Merck Sharp & Dohme Corp.||July 4 2012||Phase 3|
|NCT03376594||Completed||Allergic Rhinitis||Thammasat University||July 30 2017||Phase 2|
|NCT01916980||Completed||Eczema|Dermatitis|Dermal Pruritus||Merck Sharp & Dohme Corp.||August 27 2013||Phase 3|
|NCT01916967||Completed||Urticaria||Merck Sharp & Dohme Corp.||August 27 2013||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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