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 (58):

Cat. No. Product Name Effect Purity
  • HY-A0064
    Verapamil hydrochloride
    Inhibitor 99.98%
    Verapamil hydrochloride ((±)-Verapamil hydrochloride) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil hydrochloride also inhibits CYP3A4. Verapamil hydrochloride has the potential for high blood pressure, heart arrhythmias and angina research.
  • HY-50879
    Elacridar
    Inhibitor ≥98.0%
    Elacridar (GF120918) is a potent P-glycoprotein (Pgp) and BCRP inhibitor.
  • HY-15206
    Glibenclamide
    Inhibitor 99.79%
    Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR). Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability. Glibenclamide can induce autophagy.
  • HY-10550
    Tariquidar
    Inhibitor 98.60%
    Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM).
  • HY-14275
    Verapamil
    Inhibitor 98.82%
    Verapamil ((±)-Verapamil) is a calcium channel blocker and a potent and orally active first-generation P-glycoprotein (P-gp) inhibitor. Verapamil also inhibits CYP3A4. Verapamil has the potential for high blood pressure, heart arrhythmias and angina research.
  • HY-N2947
    Boeravinone B
    Inhibitor
    Boeravinone B, a dual inhibitor of NorA bacterial efflux pump of Staphylococcus aureus and human P-Glycoprotein, reduces the biofilm formation and intracellular invasion of bacteria. Boeravinone B act as anti-aging and anti-apoptosis phyto-molecules during oxidative stress.
  • HY-17384
    Valspodar
    Inhibitor ≥98.0%
    Valspodar (PSC 833) is a selective P-glycoprotein inhibitor that has been used as an experimental cancer treatment and chemosensitizer.
  • HY-17367A
    Atazanavir sulfate
    Modulator 99.94%
    Atazanavir (BMS-232632) sulfate, a highly selective HIV-1 protease inhibitor, is the first protease inhibitor approved for once-daily administration. Atazanavir sulfate is a substrate and inhibitor of CYP3A4, and an inhibitor and inducer of P-glycoprotein (P-gp). Atazanavir sulfate is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM.
  • HY-11018
    Risperidone
    Inhibitor 98.01%
    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-50671
    Zosuquidar trihydrochloride
    Inhibitor 99.79%
    Zosuquidar (RS 33295-198) trihydrochloride is an inhibitor of P-glycoprotein with a Ki value of 59 nM.
  • HY-13646
    Encequidar
    Inhibitor ≥98.0%
    Encequidar (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein.
  • HY-107212
    Selamectin
    Inhibitor 99.89%
    Selamectin, a semi-synthetic macrocyclic lactone, is a potent parasiticide and anthelminthic. Selamectin activates glutamate-gated chloride channels in neurons and pharyngeal muscles to prevent heartworm, Lymphatic filariae, and nematode infection. Selamectin is also a potent P-glycoprotein substrate and a P-glycoprotein inhibitor with an IC50 of 120 nM.
  • HY-50880
    Elacridar hydrochloride
    Inhibitor 99.73%
    Elacridar hydrochloride (GF120918A) is a potent P-glycoprotein (Pgp) and BCRP inhibitor.
  • 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-10550A
    Tariquidar methanesulfonate, hydrate
    Inhibitor 98.38%
    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-N0797
    (20S)-Protopanaxadiol
    Inhibitor ≥98.0%
    20S-protopanaxadiol (aPPD) is a metabolite of ginseng saponins, inhibits Akt activity and induces apoptosis in various tumor cells.
  • HY-N0450
    Sinapine thiocyanate
    Inhibitor ≥98.0%
    Sinapine thiocyanate is an alkaloid isolated from seeds of the cruciferous species. Sinapine thiocyanate exhibits anti-inflammatory, anti-oxidant, anti-tumor, anti-angiogenic and radio-protective effects. Sinapine thiocyanate is also an acetylcholinesterase (AChE) inhibitor and can be used for the research of Alzheimer’s disease, ataxia, myasthenia gravis, and Parkinson’s disease.
  • HY-13646A
    Encequidar mesylate
    Inhibitor 99.90%
    Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
  • HY-15255
    Zosuquidar
    Inhibitor 98.33%
    Zosuquidar (LY335979) is an inhibitor of P-glycoprotein with a Ki value of 59 nM.
  • HY-17013A
    Dofequidar fumarate
    Inhibitor 98.40%
    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.
Isoform Specific Products

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