Cat. No.: HY-B0801

Fexofenadine

(Synonyms: MDL-16455; Terfenadine carboxylate)

5 Cited Publications

Customer Review

Based on 5 publication(s) in Google Scholar

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.

Purity: 99.84%
CAS No.: 83799-24-0
Formula: C₃₂H₃₉NO₄
Molecular Weight:501.66

Storage:

Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month

Fexofenadine Chemical Structure

CAS No.: 83799-24-0

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (5)
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

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

All Histamine Receptor Isoforms :

Cellular Effect

Cell Line	Type	Value	Description	References
CHO	IC₅₀	23 μM Compound: Fexofenadine	Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1 Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1	[PMID: 12729675]
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	[PMID: 19362477]
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: 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]
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]
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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 83799-24-0
Appearance Solid
Molecular Weight 501.66
Formula C₃₂H₃₉NO₄
Color 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
Synonyms

MDL-16455; Terfenadine carboxylate
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

Publications (5)

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Journal Impact Factor

Pharmacol Res

Organic anion-transporting polypeptide 2B1 knockout and humanized mice; insights into the handling of bilirubin and drugs. [Abstract]

2023 Apr:190:106724. PMID: 36907287
Adv Mater Technol

2023 Jan 29.
Int Immunopharmacol

Fexofenadine protects against lipopolysaccharide-induced acute lung injury by targeting cytosolic phospholipase A2. [Abstract]

2023 Mar:116:109637. PMID: 36764283
Drug Metab Dispos

Identification of selective substrates and inhibitors of the major human renal uptake transporters. [Abstract]

2025 Mar;53(3):100046. PMID: 40024137
Biomed Pharmacother

Interplay of OATP1A/1B/2B1 uptake transporters and ABCB1 and ABCG2 efflux transporters in the handling of bilirubin and drugs. [Abstract]

2024 Jun:175:116644. PMID: 38692057

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (275 KB)
SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Watanabe N, et al. The effects of fexofenadine on eosinophilia and systemic anaphylaxis in mice infected with Trichinella spiralis. Int Immunopharmacol. 2004 Mar;4(3):367-75. [Content Brief]

[2]. Park IH, et al. Histamine Promotes the Release of Interleukin-6 via the H1R/p38 and NF-κB Pathways in Nasal Fibroblasts. Allergy Asthma Immunol Res. 2014 Nov;6(6):567-72. [Content Brief]

[3]. Ming X, et al. Vectorial transport of fexofenadine across Caco-2 cells: involvement of apical uptake and basolateral efflux transporters. Mol Pharm. 2011 Oct 3;8(5):1677-86. [Content Brief]

Calculators

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Fexofenadine

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Publications Citing Use of MedChemExpress (MCE) Fexofenadine

All Histamine Receptor Isoforms