CYP450 InhibitionADME Services

At Analiza, we understand that timelines and budgets are tight so we’ve coupled high resolution accurate mass Q-TOF MS with HPLC to help you do more with less. Our cytochrome P450 (CYP450) assay will help you understand the potential drug-drug interaction liabilities of your compounds. Full-scan data is acquired, from which narrow window extracted ion chromatograms are generated, producing quantitative data equivalent to that obtained by HPLC-MS/MS without the time-consuming process of developing distinct, MS methods for each test article. 

The streamlined CYP450 work flow means data is returned to you in as little as 72 hours, enabling you to guide structural modifications, predict in vivo performance, develop structure-metabolic stability relationships, and triage compounds for further studies in real time.

In vitro data is often ambiguous due to low compound solubility frequently observed during the discovery process.  The use of a cosolvent minimizes precipitation and reduces non-specific binding to plastics, allowing accurate data to be delivered for a higher percentage of compounds.

assay requirements

Compound Requirements

  • 10 μL of 10 mM stock solution

Test Compound Concentration

  • Screening: 10 or 25 μM
  • IC50: 0, 0.1, 0.25, 1, 2.5, 10, 25 μM

TDI Pre-Incubation Time

  • 30 min
  • Other times available

CYP Isoforms

  • CYP1A2: (Phenacetin)
  • CYP2D6: (Dextromethorphan)
  • CYP3A4: (Midazolam)
  • CYP2C9: (Diclofenac)

Analysis Method

  • HPLC-MS

Data Delivery

  • Screening: Percent Inhibition
  • IC50: 7 point IC50
  • 3A4 TDI-Single Pt: Percent inhibition after pre-incubation
  • 3A4 TDI-IC50: 7 Pt. IC50, Shifted IC50

Cost

Quotes available upon request for:

  • Screening (per isoform)
  • IC50 (per isoform)
  • 3A4 TDI: Single Point
  • 3A4 TDI IC50

our experts are available to answer your questions

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