CYP2B6 inhibition (HLM, bupropion substrate) - US

Item: 2065

Price: Login to View Pricing

Status: Available

ADD TO CART

OVERVIEW

DOCUMENTS/REFERENCES

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:

CYP2B6

Uniprot Number:

P20813

Gene Name:

CYP2B6

Gene ID:

1555

Gene Aliases:

CPB6|CYPIIB6

Organism:

Human

Construct Details:

Microsomes

Tissue:

Liver

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:

100 µM Bupropion

Incubation:

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

Test Sample Requirements:

Minimum for 1) Screen: 100 μl of 10 mM stock -OR- 1 to 2 mg (pre-weighed). 2) Dose Response: 250 μl of 10 mM stock -OR- 1.5 to 2 mg (pre-weighed).

Turnaround Time

Standard:

10 Business Days

Clinical Relevance

Adverse / Beneficial Action:

Inhibition may result in altered drug metabolism.

Additional Information

Brand:

Cerep

Testing Location:

USA - St Charles, MO