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.

BMO kits for for rapid metabolite synthesis

BMO Kits are a revolutionary way to screen, optimize and produce metabolites directly from drug candidates. The kit exploits an optimized panel of catalytic chemical reaction conditions using organometallic catalysts in a multi-well parallel format. I already introduced Phase I kits in January on this blog (here’s the link to that post…).  Today, I am glad to talk about the new O-Glucuronidation Kit.

How does it work? What are the benefits? Just read on and get in contact if you have any questions!

Identify reaction conditions that producethe glucuronide adduct of a drug compound

  • Eliminate costly synthetic chemistries
  • Produce O-Glucuronides in a few days
  • Rapidly & inexpensively screen reactions leading to metabolite
  • Fast & cost-effective O-Glucuronide production in milligram quantities
  • Easily implement – compatible with existing workflow

Two Step Synthesis of Phase 2 Metabolites

 1) Coupling with Glucuronidation Reagent
O glucuronidation step 12) De-Protection with NaOH/MeOH Solution
O glucuronidation step 2

State-of-the-art Biomimetic technology to mimic UDP-Glucuronyl Transferase

O glucuronidation example 1
O glucuronidation example 2

Kit Features

  • Derived from the Koenigs-Knorr reaction
  • Innovative panels of chemical reaction conditions utilizing reagents in a multi-well, parallel format
  • 8 reaction conditions and 2 reaction conditions using BF3
  • 4 different salts (Ag2CO3, Ag2O, Cs2CO3 and Na2CO3)
  • 2 different solvents

Products

Written by Jean-François Têtu, PhD
Jean-François Têtu is Sales & Marketing Manager at tebu-bio He also fervently defends and promotes anything from his home territory, the north of France.