Fexofenadine
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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 純度: 99.84%
- CAS 番号: 83799-24-0
- 分子式: C32H39NO4
- 分子量:501.66
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保管条件:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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MedChemExpress（MCE）の使用を引用している文献 Fexofenadine
MoreHistamine Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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H1 Receptor |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | IC50 |
23 μM
Compound: Fexofenadine
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Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1
Inhibition of K+ channel activity in CHO cells expressing HERG Kv11.1
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[PMID: 12729675] |
| CHO-K1 | IC50 |
78 nM
Compound: 37
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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
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[PMID: 19362477] |
| CHO-K1 | IC50 |
78 nM
Compound: Fexofenadine
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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
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[PMID: 21470866] |
| CHO-K1 | IC50 |
78 nM
Compound: 37
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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
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10.1016/j.bmcl.2009.03.124 |
| HEK293 | IC50 |
23 μM
Compound: 42, Fexofenadine
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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
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[PMID: 16931010] |
| HEK293 | IC50 |
65 μM
Compound: Fexofenadine
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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
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[PMID: 19260734] |
| HEK293 | IC50 |
23 μM
Compound: figure 2, R2C2
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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
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[PMID: 22542010] |
| L929 | IC50 |
>100 nM
Compound: rac-2
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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
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[PMID: 19660947] |
| L929 | IC50 |
>100 μM
Compound: rac-2
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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
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[PMID: 19660947] |
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.
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Cell Line:Nasal fibroblasts
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Concentration:100 μM
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Incubation Time:1 hour
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Result:Blocked pp38 activation in histamine-induced nasal fibroblasts, showed histamine-induced IL-6 production mediated by the p38 pathway.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice infected with Trichinella spiralis[1]
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Dosage:5, 10 and 20 mg/kg
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Administration:Oral administration; 5, 10 and 20 mg/kg; once daily; 3 weeks
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Result:Inhibited eosinophilia in a dose-dependent manner.
Suppressed the decrease in rectal temperature (p<0.01), a marker for systemic anaphylaxis.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 83799-24-0
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性状 Solid
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分子量 501.66
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分子式 C32H39NO4
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Color White to light yellow
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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
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別名
MDL-16455; Terfenadine carboxylate
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (5)
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Journal Impact Factor
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Most Recent
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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 -
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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
純度とドキュメンテーション
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データシート (275 KB)
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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)
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取扱説明書 (2659 KB)
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Fexofenadine 関連分類
HY-B0801 関連分類
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