Fexofenadine HCl

製品コードS3208 バッチS320802

印刷

化学情報

Chemical Structure Synonyms MDL 16455A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C32H39NO4.HCl
分子量 538.12 CAS No. 153439-40-8
Solubility (25°C)* 体外 DMSO 100 mg/mL (185.83 mM)
Ethanol 100 mg/mL (185.83 mM)
Water Insoluble
* <1 mg/ml means slightly soluble or insoluble.
* 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.

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生物活性

製品説明 Fexofenadine (MDL 16455A) inhibits histamine H1 receptor with IC50 of 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]

プロトコル(参考用のみ)

キナーゼアッセイ Binding assay
Cerebellum that is used for the binding experiments is homogenised with an Ultra-Turrax (setting 5 for 20 sec) in 30 volumes of ice-cold 50mM phosphate buffer (pH 7.5) and centrifuged at 3 ?105 g for 10 minutes (4 ℃). The resulting pellet is resuspended in 30 volumes of ice-cold 50 mM phosphate buffer (pH 7.5). Competition assays are performed in triplicate, in a final volume of 1 mL. Each assay tube contained the following: 0.1 mL of the different concentrations of the displacer drugs (0.1 mL of vehicle if no competing drug is added) and 0.1 mL of [3H]-pyrilamine (NEN, 23 Ci/mmol) in buffer (final concentration 1 nM). Nonspecific binding is determined using 10 μM of cold astemizole.

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Histamine Receptor Antagonists, Loratadine and Azelastine, Sensitize P-gp-overexpressing Antimitotic Drug-resistant KBV20C Cells Through Different Molecular Mechanisms. [ Anticancer Res, 2019, 39(7):3767-3775] PubMed: 31262903
Bafetinib (INNO-406) reverses multidrug resistance by inhibiting the efflux function of ABCB1 and ABCG2 transporters [Zhang YK, et al. Sci Rep, 2016, 10.1038/srep25694] PubMed: 27157787

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

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