OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Drug transporters are from two major transporter superfamilies, ABC (ATP binding cassette) and SLC (solute carrier) transporters. Multidrug And Toxin Extrusion Protein 1 (MATE-1) belongs to SLC superfamily and plays a role in the active renal secretion of drugs. This cell-based assay assesses if test compounds are substrates of target transporters. Test compounds are detected via LC-MS/MS. Transporter cell lines and Wild Type (WT) control cells are treated with compounds to determine specific transporter uptake compared to passive permeability in WT control cells. The percent of decrease of test compound uptake in a transporter cell line by the transporter specific inhibitor is determined. A test compound is considered as a substrate if (1) an uptake ratio of ≥ 2 for the test compound in transporter cell line versus WT cells; and (2) a known inhibitor at 10X of IC50 decreases uptake of test compound ≥ 50% in transporter cells.
Family:
Transporter
Sub Family:
SLCO / Organic Anion
Class:
SLC
Organism:
Human
Construct Details:
Full length, recombi
Cell Type:
CHO-K1
Assay Information
Assay Type:
Functional
Assay Sub Type:
Cell Based
Functional Mode:
Antagonist
Testing Information
Criteria For Significance:
uptake ratio > 2 and inhibition by an inhibitor > 50%
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:
20 Business Days
Additional Information
Brand:
Cerep
Testing Location:
USA - St Charles, MO
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