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Loratadine Histamine Receptor antagonist

Cat.No.S1358

Loratadine is a histamine H1 receptor antagonist, used to treat allergies. This compound also acts as a selective inhibitor of B(0)AT2 with IC50 of 4 μM.
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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

Ethanol : 77 mg/mL

DMSO : 17 mg/mL (44.4 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

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In vivo
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Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 382.88 Formula

C22H23ClN2O2

Storage (From the date of receipt)
CAS No. 79794-75-5 Download SDF Storage of Stock Solutions

Synonyms SCH29851 SMILES CCOC(=O)N1CCC(=C2C3=C(CCC4=C2N=CC=C4)C=C(C=C3)Cl)CC1

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Mechanism of Action

Targets/IC50/Ki
H1 receptor
B(0)AT2
4 μM
In vitro

Lororatadine 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. This compound 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. It also inhibits (10-40%) histamine, LTC4, and PGD2 release from purified HLMC (16-68%) activated by anti-Fc epsilon RI. This chemical 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. It 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). This compound 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. It inhibits rhinovirus-induced ICAM-1 upregulation in both primary bronchial or transformed (A549) respiratory epithelial cells. This chemical 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.

References
  • [4] https://pubmed.ncbi.nlm.nih.gov/9349397/
  • [5] https://pubmed.ncbi.nlm.nih.gov/11496238/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-08-14)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT07661459 RECRUITING
Solid Tumors
Val Adams
2026-06-26 PHASE2
NCT05263206 RECRUITING
Pruritus
Sanofi
2022-02-15 PHASE3
NCT07300735 RECRUITING
Hematologic Malignancy; Neutropenia; Bone Pain
Alexandria University
2025-03-01
NCT07532993 NOT_YET_RECRUITING
Allergic Rhinitis (AR)
Liaquat National Hospital & Medical College
2026-09 PHASE4
NCT07101445 RECRUITING
Multiple Myeloma
Emory University
2025-09-24 PHASE4
NCT05421416 RECRUITING
Stem Cell Transplant Complications
AHS Cancer Control Alberta
2024-11-28 PHASE2

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