1. Signaling Pathways
  2. Membrane Transporter/Ion Channel
  3. P-glycoprotein

P-glycoprotein

P-glycoprotein (P-gp) also known as multidrug resistance protein 1 (MDR1) is an important protein of the cell membrane that pumps many foreign substances out of cells. More formally, it is an ATP-dependent efflux pump with broad substrate specificity. P-gp is extensively distributed and expressed in the intestinal epithelium where it pumps xenobiotics (such as toxins or drugs) back into the intestinal lumen, in liver cells where it pumps them into bile ducts, in the cells of the proximal tubular of the kidney where it pumps them into urine-conducting ducts, and in the capillary endothelial cells comprising the blood–brain barrier and blood-testis barrier, where it pumps them back into the capillaries. Some cancer cells also express large amounts of P-gp, which renders these cancers multi-drug resistant. P-gp is an ATP-dependent drug efflux pump for xenobiotic compounds with broad substrate specificity. It is responsible for decreased drug accumulation in multidrug-resistant cells and often mediates the development of resistance to anticancer drugs. This protein also functions as a transporter in the blood–brain barrier.

P-glycoprotein Related Products (34):

Cat. No. Product Name Effect Purity
  • HY-50879
    Elacridar Inhibitor 98.47%
    Elacridar is a potent P-glycoprotein (Pgp) and BCRP inhibitor.
  • HY-17384
    Valspodar Inhibitor 99.27%
    Valspodar is a selective P-glycoprotein inhibitor that has been used as an experimental cancer treatment and chemosensitizer.
  • HY-17367A
    Atazanavir sulfate Inhibitor 99.64%
    Atazanavir sulfate (BMS-232632 sulfate) is a highly selective HIV-1 protease inhibitor for the treatment of HIV infection, and is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate (BMS-232632 sulfate) is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp).
  • HY-50671
    Zosuquidar trihydrochloride Inhibitor 98.75%
    Zosuquidar trihydrochloride is an inhibitor of P-glycoprotein with a Ki value of 59 nM.
  • HY-11018
    Risperidone Inhibitor 99.16%
    Risperidone is a serotonin 5-HT2 receptor blocker, P-Glycoprotein inhibitor and potent dopamine D2 receptor antagonist, with Kis of 4.8, 5.9 nM for 5-HT2A and dopamine D2 receptor, respectively.
  • HY-128685
    FD 12-9 Inhibitor
    FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity.
  • HY-112912
    P-gp modulator 1
    P-gp modulator 1 is a high affinity, orally available modulator of P-glycoprotein (Pgp), can reverse the Pgp-mediated multidrug resistance ((MDR).
  • HY-101511
    TTT-28 Inhibitor
    TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity, which reverses the ATP-binding cassette sub-family B member 1 (ABCB1)-mediated Multidrug resistance (MDR) by selectively blocking the efflux function of ABCB1.
  • HY-10550
    Tariquidar Inhibitor 98.57%
    Tariquidar is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1±0.9 nM).
  • HY-10550A
    Tariquidar methanesulfonate, hydrate Inhibitor 98.02%
    Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM.
  • HY-15255
    Zosuquidar Inhibitor 98.33%
    Zosuquidar (LY335979) is a potent negative modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM.
  • HY-13646
    Encequidar Inhibitor 98.12%
    Encequidar (HM30181) is a potent and selective inhibitor of P-glycoprotein.
  • HY-N0450
    Sinapine thiocyanate Inhibitor 98.32%
    Sinapine thiocyanate is an alkaloid from seeds of the cruciferous species which shows favorable biological activities such as antioxidant and radio-protective activities.
  • HY-N5077
    Sinapine Inhibitor 99.72%
    Sinapine is an alkaloid from seeds of the cruciferous species which shows favorable biological activities such as antioxidant and radio-protective activities.
  • HY-N0144
    Piperine Inhibitor 98.94%
    Piperine, a natural alkaloid isolated from Piper nigrum L, inhibits P-glycoprotein and CYP3A4 activities with an IC50 value of 61.94±0.054 μg/mL in HeLa cell.
  • HY-N0797
    (20S)-Protopanaxadiol Inhibitor >98.0%
    (20S)-Protopanaxadiol (20-Epiprotopanaxadiol) is an aglycon metabolic derivative of the protopanaxadiol-type ginseng saponin; apoptosis inducer.
  • HY-17013A
    Dofequidar fumarate Inhibitor 99.99%
    Dofequidar fumarate(MS-209 fumarate), an orally active quinoline compound, has been reported to overcome MDR by inhibiting ABCB1/P-gp, ABCC1/MDR-associated protein 1, or both.
  • HY-19626
    NSC23925 Inhibitor 99.23%
    NSC23925 is a novel, selective and effective P-glycoprotein (Pgp) inhibitor.
  • HY-106004
    Zamicastat Inhibitor 99.95%
    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor that could cross the blood-brain barrier (BBB) and cause central as well as peripheral effects. Zamicastat is also a concentration-dependent dual P-gp and BCRP inhibitor with IC50 values of 73.8 μM and 17.0 μM, respectively. Reduces high blood pressure.
  • HY-50880
    Elacridar hydrochloride Inhibitor 98.87%
    Elacridar hydrochloride (GF120918A) is a P-glycoprotein inhibitor, and has been used both in vitro and in vivo as a tool inhibitor of P-glycoprotein (Pgp) to investigate the role of transporters in the disposition of various test molecules.
Isoform Specific Products

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