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Drug transporter inhibition assays

Lead compounds Transporter inhibition activity ص帳ϴ.


  • ž FDA EMA Ǵ Դϴ.
  • Single (10 μM) Ȥ 8 (0.03, 0.1, 0.3, 1, 3, 10, 30, 100 μM) ׽Ʈ Ͽ IC50 ׷ մϴ.
  • test transporter : ABC transporters (MDR1/P-gp, BCRP), SLC transporters (OAT1, OAT3, OATP1B3, OCT2)
  • transporter , ٸ transporter ̿ 赵 մϴ.
  • recombinant cell line մϴ.
  • ҿ Ⱓ : ȸ , 3
  • ʿ  : 100 μl (10 mM in DMSO) or 2mg (solid stock)
    • Cells are seeded in a 96-well culture plate typically at 20,000 cells/well and are used on days 2 or 3 post-seeding. On the day of assay the test compound is prepared in assay buffer (HBSS-HEPES, pH 7.4), added to the cell plate, and preincubated at 37  for 15 min.
    • Subsequently substrate is added to the plate followed by 20-min incubation at 37 .The plate is then washed with cold assay buffer followed by fluorescence reading for assays with fluorogenic substrates.
    • For assays with radioactive substrates the cells are lysed using NaOH solution (0.2 N) followed by liquid scintillation counting.

Ref. No. Transporter  Cell line  Substrate  Reference inhibitor
1324 P-gp  MDR1-MDCKII  Calcein AM  Verapamil
3633 BCRP  BCRP-CHO  Hoechst 33342  KO143
3878 MRP1  MRP1-HEK  Calcein AM  MK571
3879 MRP2  MRP2-HEK  CDCF  MK571
3880 MRP3  MRP3-HEK  CDCF  MK571
3660 OATP1B1  OATP1B1-CHO  Fluorescein methotrexate  Rifampicin
3661 OATP1B3  OATP1B3-CHO  Fluorescein methotrexate  Rifampicin
3658 OAT1  OAT1-CHO  6-carboxyfluorescein  Probenecid
3659 OAT3  OAT3-CHO  6-carboxyfluorescein  Probenecid
3746 OCT1 OCT1-CHO  ASP+  Verapamil
3726 OCT2 OCT2-CHO  ASP+  Verapamil
3656 ASBT  ASBT-CHO  3H-taurocholic acid  Glycochenodeoxycholate
3657 NTCP  NTCP-CHO  3H-taurocholic acid  Cyclosporin A

Inhibition profiles of FDA and EMA recommended transporters
Inhibition of transport of fluorogenic substrates by transporter inhibitor reference compounds (% of control response)

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