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Email: fidelta@glpg.com

Background:
Screening of plasma and blood stability provides useful information:
•     to prioritize compounds for in vivo studies
•     to alert researchers to the potential liabilities of key pharmacophores, so that structural
      modifications could be applied to improve the stability of test compounds
   Assay description

   Source
   plasma: mouse, rat, dog, rabbit, monkey, human
   blood: mouse, rat, human

   Compound concentration
   5µM (0.5% DMSO)

   Compound requirements
   50µl of 10mM stock solution or
   1-2 mg of dry matter

   Incubation details
   1h at 37ºC or
   0-24h with multiple time-points

   Assay controls
   propranolol, eucatropine, benfluorex  (Figure 1)

   Detection method
   LC-MS/MS with internal standard

   Results
   % remaining or
   half-life (multiple time-points assay)
Figure 1. Plasma stability of reference compounds
in 3 different species

Assay details adjustable to client’s and/or project specific requests

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