Fexofenadine HCl

For research use only.

Catalog No.S3208 Synonyms: MDL 16455A

2 publications

Fexofenadine HCl Chemical Structure

Molecular Weight(MW): 538.12

Fexofenadine inhibits histamine H1 receptor with IC50 of 246 nM.

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10mM (1mL 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.
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]


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


CAS No. 153439-40-8
Storage powder
in solvent
Synonyms MDL 16455A
Smiles Cl.CC(C)(C(O)=O)C1=CC=C(C=C1)C(O)CCCN2CCC(CC2)C(O)(C3=CC=CC=C3)C4=CC=CC=C4

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT03796377 Completed Drug: St Johns Wort Extract|Drug: Rivaroxaban Drug Interaction Study University Hospital Inselspital Berne|Bayer February 13 2019 Phase 1
NCT03078777 Recruiting Drug: Fexofenadine Hemodialysis Lawson Health Research Institute November 29 2017 Phase 4
NCT02360644 Active not recruiting Dietary Supplement: Cholecalciferol Chronic Kidney Diseases|Deficiency Vitamin D University of Colorado Denver|University of Pittsburgh|National Institute of General Medical Sciences (NIGMS) October 2014 Not Applicable

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Histamine Receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID