P-gp (MDR1) (ABCB1)
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P-gp (MDR1) Transporter: ABCB1
About P-gp (MDR1)
The P-gp transporter is an efflux transporter that is encoded by the ABCB1 gene. P-gp is also known as P-glycoprotein and the Multi-Drug Resistance transporter 1 (MDR1). P-gp (MDR1) is expressed in many tissues of the body including in the kidney on the apical side of the intestinal lumen, the apical side of the bile canaliculus in liver hepatocytes, the apical membrane of proximal tubule epithelial cells and the apical side of the capillaries in the blood brain barrier (BBB). P-gp (MDR1) serves to limit the absorption of substrates, protect them from entering the brain and also to mediate their renal and hepatic elimination.
P-gp (MDR1) Substrates
P-gp (MDR1) substrates include digoxin, loperamide, paclitaxel and fexofenadine. Most CNS active drugs are not P-gp substrates.
P-gp (MDR1) Inhibitors
P-gp (MDR1) inhibitors include verapamil, cyclosporine and quinidine .
Optivia P-gp (MDR1) Transporter Assays
Optivia offers P-gp (MDR1) substrate and inhibition assays in the gold standard model for transport: polarized mammalian cells. We offer a wide range of studies including single concentration screens up to full kinetic studies to determine the IC50 for P-gp (MDR1) inhibitors and Vmax, Km and/or IC50 for P-gp (MDR1) substrates.
The probe substrate for the Optivia P-gp (MDR1) assay is digoxin. Verapamil is the reference inhibitor. These serve as the positive controls for the P-gp (MDR1) substrate assays and the P-gp (MDR1) inhibition assays, respectively.
About P-gp (MDR1)
The P-gp transporter is an efflux transporter that is encoded by the ABCB1 gene. P-gp is also known as P-glycoprotein and the Multi-Drug Resistance transporter 1 (MDR1). P-gp (MDR1) is expressed in many tissues of the body including in the kidney on the apical side of the intestinal lumen, the apical side of the bile canaliculus in liver hepatocytes, the apical membrane of proximal tubule epithelial cells and the apical side of the capillaries in the blood brain barrier (BBB). P-gp (MDR1) serves to limit the absorption of substrates, protect them from entering the brain and also to mediate their renal and hepatic elimination.
P-gp (MDR1) Substrates
P-gp (MDR1) substrates include digoxin, loperamide, paclitaxel and fexofenadine. Most CNS active drugs are not P-gp substrates.
P-gp (MDR1) Inhibitors
P-gp (MDR1) inhibitors include verapamil, cyclosporine and quinidine .
Optivia P-gp (MDR1) Transporter Assays
Optivia offers P-gp (MDR1) substrate and inhibition assays in the gold standard model for transport: polarized mammalian cells. We offer a wide range of studies including single concentration screens up to full kinetic studies to determine the IC50 for P-gp (MDR1) inhibitors and Vmax, Km and/or IC50 for P-gp (MDR1) substrates.
The probe substrate for the Optivia P-gp (MDR1) assay is digoxin. Verapamil is the reference inhibitor. These serve as the positive controls for the P-gp (MDR1) substrate assays and the P-gp (MDR1) inhibition assays, respectively.