Puracyp is dedicated to providing high quality research with a primary focus on high volume screening of new chemical entities to identify potential inducers of P450 enzymes and ABC transporters. Puracyp’s nuclear receptor activation service utilizes either stably integrated cell lines or transiently... Show more »
Puracyp is dedicated to providing high quality research with a primary focus on high volume screening of new chemical entities to identify potential inducers of P450 enzymes and ABC transporters. Puracyp’s nuclear receptor activation service utilizes either stably integrated cell lines or transiently transfected cells harboring P450 enhancer elements in reporter gene constructs and human or animal nuclear receptors including PXR, CAR and AhR. Nuclear receptor assays currently available include those employing the CYP3A, CYP2B, P-glycoprotein or CYP1A2-DRE enhancers and promoters.
Nuclear receptors derived from various species are also available that can alleviate many animal studies and provide valuable information regarding a NCE and its potential to alter pharmacokinetic parameters. Information gained from employing human nuclear receptors can be used to predict in vivo responses from NCEs with regards to drug-drug interactions and adverse drug effects.
Puracyp’s scientists are extensively published and have been involved in human P450 metabolism research for a number of years. Presently, the company has two main divisions, products and services. Products now include kits that are all inclusive and contain our stably integrated human or rat PXR and human AhR cell lines. Puracyp also offers vials of our cryopreserved DPX2, 1A2-DRE and rPXR cells in 6 or 12 million cells per vial that can be formatted for 96 or 384 well plate analyses.
NUCLEAR RECEPTOR ACTIVATION
Screening for nuclear receptor activation is a widely used and accepted practice to predict adverse drug effects and drug-drug interactions. Moreover, assessing nuclear receptor activation meets the latest FDA guidance for industry on Drug-Drug Interactions. Receptor activation screening services... Show more »
NUCLEAR RECEPTOR ACTIVATION
Screening for nuclear receptor activation is a widely used and accepted practice to predict adverse drug effects and drug-drug interactions. Moreover, assessing nuclear receptor activation meets the latest FDA guidance for industry on Drug-Drug Interactions. Receptor activation screening services using Puracyp’s proprietary cell lines are available to identify NCEs that have the potential to activate human, rat, mouse, dog or monkey SXR/PXR, AhR and CAR.
NUCLEAR RECEPTOR ASSAYS CURRENTLY AVAILABLE
Species | Nuclear Receptor: | AhR | PXR | CAR1 | CAR3 | PPARα | PPARγ | NRF2 | ERa | GR | FXR |
---|---|---|---|---|---|---|---|---|---|---|---|
Human | + | + | + | + | + | + | + | + | + | + | |
Rat | + | + | - | + | - | - | - | - | - | - | |
Monkey (Rhesus) | - | + | - | + | - | - | - | - | - | - | |
Canine (Beagle) | + | + | - | + | - | - | - | - | - | - | |
Sheep (Ovaris Aries) | - | + | - | - | - | - | - | - | - | - |
NUCLEAR RECEPTOR SCREENS
Puracyp offers single assays or panel screens at a discounted price. Our panels are designed to address the FDA’s recent guidance that CYP2B6, CYP1A2 and CYP3A4 induction by NCEs be evaluated. Puracyp’s cells contain the promoter/enhancer of these three P450 enzymes in addition to either CAR, AhR, or PXR. Panel screens are also useful for examining species differences in P450 induction and for toxicology studies using orthologs of human nuclear receptors.
Mix and match any receptor or species ortholog to develop your own nuclear receptor activation panel. An example of the available assays to use in your study design are shown below.
Mix and match any receptor or species ortholog to develop your own nuclear receptor activation panel. An example of the available assays to use in your study design are shown below.
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