Cytochrome P450 enzymes (CYPs) have a central role in drug metabolism. Drug candidates inducing CYP expression or enzyme activity can potentially increase rate of metabolism and under-exposure of co-administered drugs. Strong CYP induction can be also a sign of hepatotoxicity.
We are pleased to offer a novel solution to study CYP and other drug metabolism related genes activity – TRAC. TRAC is a novel high-throughput solution for multiplexed expression analysis. We offer TRAC in collaboration with →Plexpress, the developers of the patented TRAC method and located next door to SBW in Viikki, Helsinki. Our combined service allows more efficient screening of gene expression induction of CYPs and other ADME related transcripts in human primary hepatocytes or HepaRG cells by the drug compounds. The gene expression analysis can also be combined with LC/MS-MS determination of →CYP metabolites as well as →CYP identification and CYP inhibition.
Compared to other methods, TRAC offers
• Significant cost savings in gene expression screening compared to qPCR
• All relevant CYP genes readily available as a multiplexed assay
• Multiplexing capacity of up to 30 genes/sample
• Reliable detection: excellent repeatability with CVs <10%, good correlation with qPCR • Reliable normalization: housekeeping genes are analyzed from the same sample as the target genes • Detection directly from cell lysates: no need for RNA extraction or cDNA conversion
The transcripts detected by the CYP TRAC service include
Cytochrome P450 family enzymes
• Cyp1A1, Cyp1A2, Cyp2A6, Cyp2B6, Cyp2C8, Cyp2C9, Cyp2C19, Cyp2D6, Cyp2E1, Cyp3A4, CYP11A, CYP11B2, CYP17 and CYP19
• 17bHSD1, 17bHSD4, 3bHSD2, Por, Sult2A1, Ugt1A1, HMOX1, ABCA, ABCC2
Expression profiles of CYP3A4, CYP1A2 and CYP2B6 analyzed by TRAC in differently treated primary
hepatocytes from 3 donors. Error bars represent the standard error of the mean (SEM). Expression levels are
presented as fold change to vehicle treatment (DMSO). Data by Plexpress.
Promotional offer for CYP induction by TRAC
We offer a special 25% discount on CYP induction by TRAC studies, which have been ordered during February-March, 2012. The studies are conducted either by using cryopreserved primary hepatocytes or HepaRG cells. The detected transcripts include those listed above. Further customization to the study protocols are available, like used cell systems and detected transcripts.
The promotional offer also includes 25% discount on CYP inhibition and CYP identification studies, when ordered together with CYP TRAC.
Please contact us for more information and case studies comparing TRAC to other methods.