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Our Cytochrome P450 (CYP) inhibition assay (IC50) services help to understand the properties of a New Chemical Entity's (NCE) drug-drug reaction. CYP P450 assay also aims to understand the drug's enzymatic conversion into one or more than one metabolite. The understanding of the metabolic pathway of the drug helps to assess the nature of the drug. CYP P450 inhibition data help medicinal chemists to enhance the properties of the drug and design strategies to investigate clinical DDI studies.

Our CYP Inhibition AssayP450 Services Include:

Cytochrome P450 (CYP) inhibition assay protocol (IC50)

Test system HLM probed with substrates specific for each isoform
Isoforms 3A4, 2D6, 2C9, 1A2, 2C8, 2C19 and 2B6
Test concentrations 50 µM / IC50 concentrations
Incubation time 10 min (3A4), 20 min (2D6, 2C9, 1A2, 2C8, 2C19, 2B6)
Test system Human liver microsomes
Analysis LC-MS/MS method
Deliverables Percent inhibition and/or IC50

CYP Inhibition Profile of AU-0000

Cytochrome P450 time-dependent inhibition (kinact/KI)

Design Test compound pre-incubated in HLM probed with isoform-specific substrates to monitor the IC50 shift
Isoforms 3A4, 2D6, 2C9, 2C19, 1A2
Test concentrations Compound dependent, six inactivator concentrations
Incubation time 5 min with 6 pre-incubation time points
Test system Human liver microsomes
Analysis LC-MS/MS method
Deliverables Percent inhibition, IC50, and IC50 shift

 

TDI CYP 3A4: Azamulin
Historical Data CYP3A4 Inhibition
TDI CYP 3A4 (Testosterone) of AU-0000
CYP Chart

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CYP Induction Study Protocol

Test System Cryopreserved inducible human hepatocytes
Method mRNA estimation
Test concentrations 50, 30 & 10µM
Incubation time 72 hours with daily dosing
Test system Plateable human hepatocytes
Deliverables Fold Induction and/ or % induction with respect to positive control

CYP Phenotyping Study

  • Test System: Human recombinant CYPs
  • Relative contribution of individual CYP isoforms to the metabolism of the parent compound estimated

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