1. GPCR/G Protein Neuronal Signaling Immunology/Inflammation
  2. Histamine Receptor
  3. Fexofenadine

Fexofenadine  (Synonyms: MDL-16455; Terfenadine carboxylate)

Cat. No.: HY-B0801 Purity: 99.84%
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Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research.

For research use only. We do not sell to patients.

Fexofenadine Chemical Structure

Fexofenadine Chemical Structure

CAS No. : 83799-24-0

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Based on 4 publication(s) in Google Scholar

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Description

Fexofenadine (MDL-16455) is an orally active and nonsedative H1 receptor antagonist. Fexofenadine can be used in allergic rhinitis and chronic idiopathic urticarial research[1][2][3].

IC50 & Target[1]

H1 Receptor

 

Cellular Effect
Cell Line Type Value Description References
CHO-K1 IC50
78 nM
Compound: Fexofenadine
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
Displacement of [3H]pyrilamine from human histamine H1 receptor expressed in CHO-K1 cells after 60 mins by scintillation counting
[PMID: 21470866]
CHO-K1 IC50
78 nM
Compound: 37
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
Displacement of [3H]pyrilamine from human recombinant histamine H1 receptor expressed in CHOK1 cells by scintillation counting
10.1016/j.bmcl.2009.03.124
HEK293 IC50
23 μM
Compound: figure 2, R2C2
Inhibition of human Erg expressed in HEK293 cells assessed as rubidium efflux after 4 hrs by atomic absorbance spectrometric analysis
Inhibition of human Erg expressed in HEK293 cells assessed as rubidium efflux after 4 hrs by atomic absorbance spectrometric analysis
[PMID: 22542010]
HEK293 IC50
23 μM
Compound: 42, Fexofenadine
Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay
Inhibition of human ERG potassium channel in HEK293 cells by patch clamp assay
[PMID: 16931010]
HEK293 IC50
65 μM
Compound: Fexofenadine
Inhibition of human ERG expressed in HEK293 cells by whole cell patch clamp method
Inhibition of human ERG expressed in HEK293 cells by whole cell patch clamp method
[PMID: 19260734]
L929 IC50
> 100 nM
Compound: rac-2
Inhibition of human ERG in L929 cells by whole cell patch-clamp assay
Inhibition of human ERG in L929 cells by whole cell patch-clamp assay
[PMID: 19660947]
L929 IC50
> 100 μM
Compound: rac-2
Inhibition of human ERG in L929 cells at 10 uM by whole cell patch-clamp assay
Inhibition of human ERG in L929 cells at 10 uM by whole cell patch-clamp assay
[PMID: 19660947]
In Vitro

Fexofenadine (1-100 μM; 1 h) inhibits the expression of IL-6 protein in nasal fibroblasts in a dose-dependent manner[2].
Fexofenadine (1-100 μM; 1 h) blocks phosphorylated p38 activation in histamine-induced nasal fibroblasts, but shows no effect on either pERK or pJNK[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[2]

Cell Line: Nasal fibroblasts
Concentration: 100 μM
Incubation Time: 1 hour
Result: Blocked pp38 activation in histamine-induced nasal fibroblasts, showed histamine-induced IL-6 production mediated by the p38 pathway.
In Vivo

Fexofenadine hydrochloride (oral administration; 5-20 mg/kg; once daily; 3 w) suppresses both eosinophilia and systemic anaphylaxis in C57BL/6 mice infected with T. spiralis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6 mice infected with Trichinella spiralis[1]
Dosage: 5, 10 and 20 mg/kg
Administration: Oral administration; 5, 10 and 20 mg/kg; once daily; 3 weeks
Result: Inhibited eosinophilia in a dose-dependent manner.
Suppressed the decrease in rectal temperature (p<0.01), a marker for systemic anaphylaxis.
Clinical Trial
Molecular Weight

501.66

Formula

C32H39NO4

CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

OC(C1=CC=CC=C1)(C2=CC=CC=C2)C3CCN(CCCC(C4=CC=C(C(C(O)=O)(C)C)C=C4)O)CC3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Purity & Documentation

Purity: 99.84%

References
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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