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CYP450 Inhibition

Fast, Accurate and Affordable

Whether you’re tight on budget, time, or internal capacity, Analiza offers a CYP450 inhibition study to meet your discovery needs. We understand that different therapeutic areas and programs have different needs so we’ll work with you to identify the right screening strategy for you; maximizing your budget while enabling you to identify compound liabilities in real time.

For initial screening, single inhibitor concentration provides relevant outcomes and is ideal for early discovery. However, if the IC50 values are much smaller or larger than the concentration tested it may difficult to distinguish between Time dependent Inhibition (TDI) and direct inhibition. With 3A4 responsible for the vast majority of clinically relevant drug-drug interactions, Analiza offers single point and 7 pt. IC50 CYP3A4 TDI studies.

3A4 TDI Data returned in 72 hours or less


Assay Protocol

Compound Requirements

  • 25 µL of 10mM 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: (Melatonin, Tacrine)
  • CYP2D6: (Dextromethorphan, Bufuralol)
  • CYP3A4: (Midazolam, Testosterone)

Analysis Method

  • LC-TOFMS

Data Delivery

  • Delivered within 72 hours
  • Screening: % Inhibition
  • IC50: 7 point IC50
  • 3A4 TDI-Single Pt: % inhibition after pre-incubation
  • 3A4 TDI-IC50: 7 Pt. IC50, Shifted IC50

Cost

  • Screening: $150.00 per isoform
  • IC50: $400.00 per isoform
  • 3A4 TDI: Single Pt: $300.00
  • 3A4 TDI IC50: $1,000.00
At-a-glance
Target
Method
LC-TOFMS
Target
72 Hours
Guaranteed turn around time after receiving your compound
Target
$150
starting price
Target
25µL
of 10mM DMSO stock solution

Physchem Services •  LogD / Log P •  Aqueous Solubility •  pKa •  Chemical Stability •  XRPD •  Accurate Mass
ADME Services •  Microsomal Stability •  CYP450 Inhibition •  PAMPA •  BBB Permeability
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