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:
ABCB
Class:
ABC
Protein Name:
P-gp
Uniprot Number:
P08183
Protein Aliases:
multidrug resistance protein 1
Gene Name:
ABCB1
Gene ID:
5243
Gene Aliases:
P-gp|CD243|GP170|ABC20
Organism:
Human
Construct Details:
Full length, recombi
Cell Type:
MDCKII
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Detection Method:
Fluorimetry
Measured Response:
Fluorescence
Testing Information
Substrate:
2 µM Calcein AM
Incubation:
35 min at 37C
Criteria For Significance:
25 % inhibition
Test Concentration / Dose:
Suggested to perform dose response study (8 concentrations; 3 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
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