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Fexofenadine HCl
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Fexofenadine HCl图片
CAS NO:153439-40-8
规格:≥98%
包装与价格:
包装价格(元)
50mg电议
100mg电议
250mg电议
500mg电议
1g电议
2g电议

产品介绍
理化性质和储存条件
Molecular Weight (MW)538.12
FormulaC32H39NO4.HCl
CAS No.153439-40-8 (HCl);
Storage-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)DMSO: 107 mg/mL (198.8 mM)
Water: 2 mg/mL (3.7 mM)
Ethanol: 107 mg/mL (198.8 mM)
Other infoChemical Name: 2-(4-(1-hydroxy-4-(4-(hydroxydiphenylmethyl)piperidin-1-yl)butyl)phenyl)-2-methylpropanoic acid hydrochloride
InChi Key: RRJFVPUCXDGFJB-UHFFFAOYSA-N
InChi Code: InChI=1S/C32H39NO4.ClH/c1-31(2,30(35)36)25-17-15-24(16-18-25)29(34)14-9-21-33-22-19-28(20-23-33)32(37,26-10-5-3-6-11-26)27-12-7-4-8-13-27;/h3-8,10-13,15-18,28-29,34,37H,9,14,19-23H2,1-2H3,(H,35,36);1H
SMILES Code: O=C(O)C(C)(C)C1=CC=C(C(O)CCCN2CCC(C(C3=CC=CC=C3)(O)C4=CC=CC=C4)CC2)C=C1.[H]Cl
SynonymsMDL 16455A; Allegra; Terfenidine carboxylate hydrochloride; Fexofenadine HCl; MDL-16-455A; MDL16455A; MDL 16 455A; Telfast
实验参考方法
In Vitro

In vitro activity: 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.


Cell Assay: Fexofenadine hydrochloride (MDL-16455 hydrochloride) (100 μM; 1 hour) effectively blocks phosphorylated p38 activation in histamine-induced nasal fibroblasts.

In VivoFexofenadine 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.
Animal modelC57BL/6 mice infected with T. spiralis
Formulation & Dosage5-20 mg/kg; oral daily
ReferencesDrugs R D. 2005;6(6):371-84; J Pharm Sci. 2005 Feb;94(2):233-9.