Fexofenadine HCl

Catalog No.S3208 Synonyms: MDL 16455A

Fexofenadine HCl Chemical Structure

Molecular Weight(MW): 538.12

Fexofenadine inhibits histamine H1 receptor with IC50 of 246 nM.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 170 In stock
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Biological Activity

Description Fexofenadine inhibits histamine H1 receptor with IC50 of 246 nM.
Targets
Histamine H1 receptor [1]
246 nM
In vitro

Fexofenadine exhibits a potent and concentration-dependent anti-anaphylactic activity with an IC50 value of 95.5nM. Fexofenadine shows only a weak competitive antagonist behaviour for the 5-HT2A receptorsfrom rat caudal artery with pA2 of 5.2. [1] All four P-gp inhibitors has a strong, concentration-dependent effect on the Papp of fexofenadine in both directions in the Caco-2 cell model. The IC50 of verapamil is 8.44 mM on the P-gp-mediated secretion of Fexofenadine. [2] Fexofenadine causes a significant increase in the QT and Tp-e intervals and receives a significant TdP score at doses greater than 100 fold its free TPC in the rabbit left ventricular wedge preparation. [3]

In vivo Fexofenadine is excreted unchanged in the urine, bile, and gastrointestinal tract, indicating minimal metabolism in rats, making it an ideal probe to study transport processes. Coadministration of Fexofenadine with Ketoconazole increases the oral exposure of Fexofenadine by 187% in rats. In contrast, coadministration of Fexofenadine with orange juice or apple juice to rats decreases the oral exposure of Fexofenadine by 31% and 22%, respectively. Increasing the quantity of orange or apple juice administered further decreases the oral exposure of Fexofenadine, by 40% and 28%, respectively. [4] Biliary excretion clearance of Fexofenadine (17 ml/min/kg) accounts for almost 60% of the total body clearance (30 ml/min/kg) in mice. Knockout mice of Mdr1a/1b P-gp does not affect the biliary excretion clearance with regard to both plasma and liver concentrations, whereas the absence of P-gp causes a 6-fold increase in the plasma concentration and 3-fold higher brain-to-plasma concentration ratio after oral administration. [5]

Protocol

Solubility (25°C)

In vitro DMSO 107 mg/mL (198.84 mM)
Ethanol 107 mg/mL (198.84 mM)
Water 2 mg/mL (3.71 mM)

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 538.12
Formula

C32H39NO4.HCl

CAS No. 153439-40-8
Storage powder
Synonyms MDL 16455A

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02908750 Not yet recruiting Non Small Cell Lung Cancer AstraZeneca|Quintiles, Inc. January 2017 Phase 1
NCT03012763 Completed Pharmacokinetics|Magnetic Resonance Imaging|Administration, Oral University Medicine Greifswald April 2016 Phase 1
NCT02391688 Completed Drug Interaction Jules Desmeules|University Hospital, Geneva November 2014 Phase 1
NCT02157558 Completed Drug Interactions Lexicon Pharmaceuticals July 2014 Phase 1
NCT02175485 Completed Rhinitis Allergic Sanofi June 2014 Phase 4
NCT02551536 Completed Allergic Rhinitis Indira Gandhi Medical College April 2014 Phase 4

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID