DISCOVER Bioactive Small Molecules for ADME/Tox

A significant number of drugs that fail in clinical trials have been associated with safety issues, including unexpected drug-drug interactions (DDI) or lack of efficacy due to poor pharmacokinetics. Thus, determining the absorption, distribution, metabolism and excretion properties, as well as the toxicity, of a lead compound is essential in the development of therapeutic drugs. The important role of ATP-binding cassette (ABC) and solute carrier (SLC) membrane transporters in ADME Tox has been demonstrated, with a particular focus on seven of the most clinically relevant transporters – OAT1, OAT3, OCT2, OATP1B1, OATP1B3, MDR1 and BCRP. As data for drug effects on these transporter targets is a regulatory requirement for any new therapeutic drug compound, it is essential to have the right tools for ADME Tox research. Several hundred approved and late-stage drugs are known inhibitors or substrates of ABC and SLC transporters. Sigma® Life Science offers bioactive small molecules, including approved drugs, to study these transporters. A selection of these compounds, including FDA-preferred substrates and inhibitors, is shown below.

In addition to tools to study membrane transporters, Sigma offers many of the drugs that are known to inhibit, induce or be metabolized by Cytochrome P450 (CYP) drug metabolizing enzymes (DMEs). The list below includes bioactive small molecules for studying CYPs, including FDA-preferred inhibitors and substrates for in vitro analysis of drug metabolizing CYP family members.

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