EMAIL THIS PAGE TO A FRIEND

Drug metabolism and pharmacokinetics

Evaluation of induction potency of new drug candidates on CYP1A2 and CYP3A4 using real-time one-step RT-PCR in primary cultures of cryopreserved human hepatocytes.


PMID 19881256

Abstract

This study evaluates the induction potency of new drug candidates on mRNA levels of CYP1A2 and CYP3A4 in primary cultures of cryopreserved human hepatocytes. Analysis was performed by quantitative real-time RT-PCR using primers and TaqMan probes. Positive controls for CYP1A2 and CYP3A4 used beta-naphthoflavone (beta-NF) and rifampicin (Rif), respectively. In the first stage of the study, the lot showing the best induction of mRNA expression CYP1A2 and CYP3A4 from among eight lots of hepatocytes was selected. In the second stage, we evaluated the levels of CYP1A2 and CYP3A4 gene expression in hepatocytes after exposure to eight NO-1886 (ibrolipim) derivatives. A combination of real-time one-step RT-PCR and primary culture of cryopreserved human hepatocytes is suitable for evaluating of induction potency of a large number of new drug candidates.

Related Materials

Product #

Image

Description

Molecular Formula

Add to Cart

N1540
NO-1886
C19H20BrN2O4P