P-gp

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.

Inhibitors

Cat.No. Product Name Information Publication Customer Review
S1481 LY335979 (Zosuquidar 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.

P-gp

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