METABOLIC STABILITY

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In order to mitigate against unacceptably high clearance it is usually necessary to identify the major metabolic pathway(s) as well as the nature of the enzymes involved. Determining clearance and stability of drugs help in dose adjustments to achieve highest efficacy with least safety issues.

Cytovier offers microsomal, S9, hepatic, plasma and recombinant enzyme stability assays to determine stability of compounds.

Stability Assay Protocol:

Test article concentration: 1  µM (other upon request) 

Incubation time: 0, 5,15, 30 and 60 minutes 

Incubation temperature: 37 C 

Number of Replicates: n = 2 

Assay condition: NADPH regeneration system 

Assay matrix: Microsomes, S9, hepatic, plasma from any species or human recombinant enzyme 

Positive controls: No regeneration system, propranolol. (other upon request). 

Analysis Method: LC/MS/MS 

Data Delivery: % parent remaining, Intrinsic clearance, Half life