Biological Information

Background Information:

Transporters are membrane proteins that control the influx and efflux of essential nutrients, ions, cellular waste, environmental toxins, and other xenobiotics such as drugs. Transporters that transport drugs across the membrane are from two major superfamilies, ABC (ATP binding cassette) and SLC (solute carrier) transporters. Eurofins has a variety of robust transporter inhibition assays to allow quick and cost-effective screening of new molecular entities (NMEs) for their interactions with these transporters. Results from these assays are important in assessing a drug’s efficacy, safety, and pharmacokinetic properties, and are also necessary for compliance with FDA and EMA guidances.

Family:

Transporter

Sub Family:

ABCG

Class:

ABC

Protein Name:

BCRP

Uniprot Number:

Q9UNQ0

Gene Name:

ABCG2

Gene ID:

9429

Gene Aliases:

EST157481|MXR|BCRP|ABCP|CD338

Organism:

Human

Construct Details:

Full length, recombi

Cell Type:

CHO-K1

Assay Information

Assay Type:

Functional

Assay Sub Type:

Cell Based

Functional Mode:

Antagonist

Detection Method:

Fluorimetry

Measured Response:

Fluorescence

Testing Information

Substrate:

5 µM HOECHST 33342

Incubation:

35 min at 37C

Criteria For Significance:

25 % inhibition

Test Concentration / Dose:

Suggested to perform dose response study (8 concentrations; 2 replicates per concentration)

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:

15 Business Days

Additional Information

Brand:

Cerep

Testing Location:

USA - St Charles, MO