10mM in DMSO for sensitive chromatographic and analytical workflows requiring minimal baseline interference.
Store at -80°C Ships Dry ice packs + Cold packs Check lot-specific COA for exact specifications.
SDS, COA, datasheet, and spec sheet available for download. Lot-specific COA accessible via lot number lookup.
Cited in 1 peer-reviewed publications across chromatography, organic synthesis, and cross-coupling reactions.
Information
Fexofenadine (MDL 16455A) inhibitshistamine H1receptor withIC50of 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. 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.
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. 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.
Cell Data
cell lines：
Concentrations：
Incubation Time：
Powder Purity:≥99%
| Isomeric SMILES | CC(C)(C1=CC=C(C=C1)C(CCCN2CCC(CC2)C(C3=CC=CC=C3)(C4=CC=CC=C4)O)O)C(=O)O.Cl |
|---|---|
| WGK Germany | 3 |
| Molecular Weight | 538.12 |
| Reaxy-Rn | 7900041 |
| Reaxys-RN_link_address | https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=7900041&ln= |
Comprehensive hazard, handling, storage, and regulatory compliance document.
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View spec sheet →| Solubility | Solubility (25°C) In vitro DMSO: 59 mg/mL (200.41 mM); Ethanol: 12 mg/mL (40.76 mM); Water: Insoluble; |
|---|---|
| Melt Point(°C) | 148-150℃ |
| 1. Yingchao Li, Xiaoyu Liu, Farong Lu, Huichao Li, Jiaming Zhang, Yawei Zhang, Wenchao Li, Weiping Wang, Miaomiao Yang, Zhining Ma, Hui Zhang, Xiaomian Zhou, Youjun Xu, Zhonggui He, Jin Sun, Tianhong Zhang, Qikun Jiang. (2024) Natural Amino Acid-Bearing Carbamate Prodrugs of Daidzein Increase Water Solubility and Improve Phase II Metabolic Stability for Enhanced Oral Bioavailability. JOURNAL OF AGRICULTURAL AND FOOD CHEMISTRY, [PMID:38569082] [10.1021/acs.jafc.4c01251] |
