Once metabolites have been identified through radio-labeling or metabolism studies, we can set you up to screen and optimize and produce metabolites directly from drug candidates through a service offered by our friends at HepatoChem. HepatoChem’s BMO (BioMimetic Oxidation) and O-Glucuronidation services are utilized for rapid metabolite synthesis for phase I or II metabolism.
Phase I Metabolism
Using an optimized panel of catalytic chemical reaction conditions using organometallic catalysts in a multi-well parallel format, the suite of cytochrome P450 enzymes (CYP) present in human hepatocytes can be mimicked, offering a unique synthetic chemical liver. This chemical liver offers the advantage of scalability of chemistry.
When a reaction condition is identified, it is optimized and scaled up to produce mg quantities of metabolites for both MS/MS and NMR.
Phase II Metabolism
Glucuronide formation can be a major avenue of drug metabolism.
O-Glucuronidation enhances the bile/plasma ratio of a metabolite relative to the parent drug. However, glucuronides are more polar and ionic than the parent drug, and while most glucuronides are inactive, they are not always lower in toxicity or inactivation. This service is intended to identify reaction conditions that produce the glucuronide adduct of a drug and produce mg quantities of O-Glucuronides quickly and inexpensively.
Benefits of the Metabolite Production Service:
- Perfect if LC-MS or chemist time is not available at your lab
- All work is performed by experienced Hepatochem platform users
- No solvents, no disposal
- Your team can remain focused on higher priority work