产品展示
Fexofenadine Hydrochloride153439-40-8盐酸非索非那定
点击次数：182发布时间：2016/7/8 16:03:59
更新日期：2024/9/19 16:50:29
所 在 地：中国大陆
产品型号：
优质供应
详细内容
盐酸非索非那定
分子式：C32H39NO4.HCl 分子量：538.13
产品描述
Fexofenadine抑制histamine H1受体，IC50为246 nM。
靶点
Histamine H1
IC50
246 nM
体外研究
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.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.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.
体内研究
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.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.
溶解性
DMSO 107 mg/mL，水 2 mg/mL，乙醇 107 mg/mL
稳定性
2年 -20°C粉状，6月-80°C溶于DMSO
