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%
Handling Instructions Technical Support

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

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Fexofenadine

Fexofenadine 화학구조

CAS No. : 83799-24-0

사이즈 가격 재고 수량
5 mg 해외재고보유
10 mg 해외재고보유
50 mg 해외재고보유
100 mg 해외재고보유
200 mg   견적 받기  
500 mg   견적 받기  

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고객리뷰

Based on 5 publication(s) in Google Scholar

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  • Biological Activity

  • 순도&문서

  • References

  • 고객리뷰

제품 설명

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 1
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 IC50
23000 1
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 IC50
23 3
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 1
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 3
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]
CHO-K1 IC50
78 1
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]
HEK293 IC50
23 3
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
65 3
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 3
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]
CHO-K1 IC50
78 1
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]
HEK293 IC50
23 3
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 3
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 3
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]
CHO-K1 IC50
78 1
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]
L929 IC50
> 100 1
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 3
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]
CHO-K1 IC50
78 1
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]
L929 IC50
>100 1
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]
HEK293 IC50
23 3
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
23 3
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
65 3
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 1
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 3
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
분자량

501.66

화학식

C32H39NO4

CAS No.
Appearance

Solid

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

선적

Room temperature in continental US; may vary elsewhere.

보관
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
순도&문서

Purity: 99.84%

References
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    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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상품명:
Fexofenadine
Cat. No.:
HY-B0801
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