Reporter Assays By Receptor

Many labs are interested in cross-species comparisons, especially contrasting human nuclear receptor activity to common laboratory animals. Determining a drug candidate’s cross-activity with human xenobiotic-sensing receptors provides important early indications of that drug’s potential for downstream drug-drug interactions. With animal studies required by the FDA, selecting the animal model that provides the most representative human-surrogate is critical to assessing a potential drug’s likelihood of unwanted effects. Cell-based assay models are crucial to help make this determination prior to entering ADMET studies.

With more than 30 ortholog assays - including rat, mouse, dog, monkey, and zebrafish - available as kits and/or services, and others available for custom development, INDIGO helps researchers screen the right animal, before trial.

INDIGO’s nuclear receptor reporter assay panels contain all materials needed to perform either 32 or 48 assays for each receptor included. PPAR, RAR, and RXR Panels are available in a 3x32-well format; ER, LXR, and TR Panels are in a 2x48-well format, all designed to fully utilize a single 96-well plate. All reagents are supplied with sufficient extra volume to accommodate the needs of performing separate groups of assays. When screening a smaller number of compounds against all variants of a receptor, INDIGO’s Assay Panel kits allow researchers to save time, cost, and risk by screening against multiple receptors in one easy-to-use kit.

In Vitro Screening for Drug-Induced Hepatotoxicity using upcyte^® Hepatocytes

The emergence of liver toxicity is major reason for the termination of clinical drug trials, as well as post-market withdrawal of approved drugs. The assay kit for in vitro screening for drug-induced hepatotoxicity allows researchers to rapidly identify those compounds that induce liver toxicity. The kit utilizes upcyte^® hepatocytes, prepared using our proprietary CryoMite^TM process, which yields high viability post-thaw and provides the convenience of immediately dispensing cells into assay plates. This all-inclusive assay kit allows users to bring processes previously available only as contract screening services into their own labs. Learn more.

Human MDR1 / P-Glycoprotein Drug Interaction Assay

Determining if a drug candidate will have incidental interactions with P-Glycoprotein (P-gp, aka MDR-1, or ABCB1) is an important component of the safety assessment process. A drug that is either a substrate or inhibitor of MDR1 transporter activity can significantly alter the rate of absorption, distribution, metabolic conversion, and eventual excretion of co-administered drugs, thereby shifting their therapeutic effects and toxicologic profiles. Because of this, assessing a new drug's potency as an interactor with P-gp, and thus its potential liability for inducing downstream drug-drug interactions, is mandated by the FDA. Our all-inclusive assay kit for the assessment of MDR1 drug interaction allows users to rapidly assess drug candidates as either inhibitors, substrates, or non-substrates of P-gp, and make critical decisions about potential drug candidates with confidence. Learn more.

Expression Profiling of Clinically Relevant CYPs Utilizing upcyte^® Hepatocytes

Assessing drug-induced changes in the expression of Cytochrome P450 (CYP) genes provides a reliable predictive indicator of altered metabolic activity in vivo. It is estimated that CYPs are involved in 70% to 80% of drugs currently on the market, making understanding their metabolic actions crucial to the drug development process. Our gene expression assay kit provides optimized reagents for the culturing and treatment of upcyte^® hepatocytes to assess drug-induced changes in the expression of seven clinically relevant CYPs: CYP3A4, CYP1A1, CYP2B6, CYP2C8, CYP2C9, CYP2C19, and CYP2E1. Learn more.