P-glycoprotein (permeability glycoprotein, P-gp, Pgp, ABCB1, ATP-binding cassette sub-family B member 1, MDR1, and PGY1) is belongs to a subfamily of ABC-transporter called MDR (Classical multidrug resistance). P-glycoprotein functions as a transporter in the blood-brain barrier with a 170 kDa polypeptide. P-gp plays a role in the elimination of drugs and metabolites in kidney and liver, and these cumulative systemic effects would eventuate in lower plasma concentrations of these drugs. P-gp inhibitors can be a kind of anti-cancer drug through reducing multidrug resistance because P-glycoprotein (Pgp), the membrane-associated protein, is overexpressed in tumor cells resulting in an enhanced ability to export drugs from the cell and multidrug resistance.
|Cat.No.||Product Name||Information||Publication||Customer Review|
|S1481||Zosuquidar (LY335979) 3HCl||LY335979 (Zosuquidar) is a potent modulator of P-glycoprotein-mediated multidrug resistance with Ki of 60 nM.||(1)|
|S8028||Tariquidar||Tariquidar (XR9576) is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM.|