OVERVIEW
DOCUMENTS/REFERENCES
Biological Information
Background Information:
Drug transporters are from two major transporter superfamilies, ABC (ATP binding cassette) and SLC (solute carrier) transporters. Organic Cation Transporter 2 (OCT2) belongs to SLC superfamily and plays a role in the active renal secretion of drugs. This cell-based assay assesses if test compounds are inhibitors of target transporters. Metformin is a known substrate of OCT1 and is used as the probe substrate in this assay. The intracellular accumulation of Metformin in OCT2 overexpressing cell line is detected via LC-MS/MS. The level of test compound transporter inhibition activity is inversely proportional to the accumulation of the probe substrate. The compound is tested at 8 concentrations, n=2, for IC50 determination in this assay.
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
Detection Method:
HPLC-MS/MS
Testing Information
Substrate:
100 µM Metformin
Incubation:
30 min pre-incubation and 20 min incubation with substrate at 37°C
Criteria For Significance:
25 % inhibition
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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