ESA Biosciences, a Magellan Biosciences company, has launched new HPLC systems designed to help speed drug-metabolism studies and support medicinal chemistry activities
The new HPLC systems have been developed to electrochemically synthesise significant quantities of difficult-to-obtain metabolites from a variety of parent compounds.
At the systems' core are new, high efficiency, high capacity electrochemical-synthesis cells.
Since the user can control the systems' oxidation capability to generate specific, desired oxidation products, they have wide utility in a variety of metabolite-generation tasks, alleviating the need to deploy precious medicinal chemistry resources to support drug-metabolism identification, while enhancing the synthesis capabilities of any laboratory.
Assessing metabolic stability and correctly identifying a compound's metabolites using various in vitro and in vivo drug-metabolism assays is a crucial step in determining a compound's suitability for drug development.
However, LC-MS, the typical technique used for metabolism studies, only reports the molecular weight of the metabolites being examined.
LCMS cannot easily determine the exact structure of a given metabolite, especially if one or more hydroxylation reactions are involved in the metabolism of the compound.
Irrefutably determining a metabolite's structure often requires synthesis of complicated metabolites by medicinal-chemistry methods - a daunting task, until now, according to ESA director of HPLC marketing, Dr Darwin Asa.
ESA's new electrochemical synthesis systems are an ideal complement to LC-MS for ADME-Tox / DMPK and other drug-metabolism operations, because they can be used to quickly and easily generate large quantities of oxidative metabolites from parent compounds.
Of particular interest to scientists evaluating the metabolic properties and toxicity of potential drugs, these systems mimic much of the oxidation capabilities of cytochrome P450, a key enzyme family that is responsible for metabolising most drugs.
Drug interactions involving the cytochrome p450 system are common, and a major cause of attrition in the drug-development process.
Understanding the metabolites generated by these enzymes is key to understanding a compound's metabolic fate.
ESA has designed two new synthesis cells to suite specific application needs.
The 5150 cell has high capacity and is preferred for low-potential ( less than 500mV) oxidation reactions, while the 5125 cell is recommended for high-potential reactions.
Although smaller in volume, the 5125 cell minimises unwanted over-oxidation reactions.
ESA Biosciences enables answers to pressing applications challenges by applying its expertise in specialty detection and electrochemistry, combined with components, kits, and reagents, for analytical laboratories, commercial diagnostics laboratories, and the clinical point-of-care setting.
ESA is a wholly owned subsidiary of Magellan Biosciences
