Biological Information

Background Information:

Cytochrome P450 (CYP) inhibition is one of the most common types of drug-drug interactions (DDI). When a drug inhibits a specific CYP isoform, it will reduce the metabolic activity toward a concomitant drug that is metabolized by this inhibited CYP isoform, resulting in the increase in the bioavailability of the victim drug, often to a point that toxicity is induced. Regulatory agencies have issued guidances recommending that all new molecular entity (NME) be screened for CYP inhibition liability, especially for CYP1A2, CYP2B6, CYP2C8, CYP2C9, CYP2C19, CYP2D6, and CYP3A4. Eurofins can determine inhibition of the major CYP enzymes using drug substrates in human liver microsomes or with fluorescent substrates and recombinant human CYP enzymes.

Family:

CYP450

Sub Family:

CYP2

Protein Name:

CYP2C9

Uniprot Number:

P11712

Gene Name:

CYP2C9

Gene ID:

1559

Gene Aliases:

P450IIC9

Organism:

Human

Construct Details:

Full length, recombi

Assay Information

Assay Type:

Biochemical

Assay Sub Type:

Enzymatic

Functional Mode:

Antagonist

Detection Method:

HPLC-MS/MS

Measured Response:

Peak Area Response

Testing Information

Substrate:

10 µM Diclofenac

Incubation:

5 min pre-incubation and 10 min with NADPH at 37°C

Test Concentration / Dose:

Assay is performed with 8 compound concentration(s) and each concentration tested using 3 replicate

Turnaround Time

Standard:

10 Business Days

Additional Information

Brand:

Cerep

Testing Location:

USA - St Charles, MO

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