2. Membrane Transporter/Ion Channel
  3. P-glycoprotein

P-glycoprotein

P-glycoprotein

Related Products

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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 (129):

Cat. No. Product Name Effect Purity
  • HY-15206
    Glibenclamide Inhibitor 99.92%
    Glibenclamide (Glyburide) is an orally active ATP-sensitive K+ channel (KATP) inhibitor and can be used for the research of diabetes and obesity[1]. Glibenclamide inhibits P-glycoprotein. Glibenclamide directly binds and blocks the SUR1 subunits of KATP and inhibits the cystic fibrosis transmembrane conductance regulator protein (CFTR)[3]. Glibenclamide interferes with mitochondrial bioenergetics by inducing changes on membrane ion permeability[4]. Glibenclamide can induce autophagy[5].
  • HY-14275
    Verapamil Inhibitor 99.96%
    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[1][2][3].
  • 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[1][2][3].
  • HY-10550
    Tariquidar Inhibitor 99.34%
    Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM)[1].
  • HY-50879
    Elacridar Inhibitor
    Elacridar is an orally active P-glycoprotein (Pgp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar can be used to examine the influence of efflux transporters on agent distribution to brain and the research of cancer[1][2].
  • HY-162373
    α-Amylase/α-Glucosidase-IN-10
    α-Amylase/α-Glucosidase-IN-10 (compound 5d) is an α-amylase and α-glucosidase inhibitor (IC50: 30.39 μM and 65.1 μM) with potential diabetes inhibitory effects. α-Amylase/α-Glucosidase-IN-10 exhibits high gastrointestinal (GI) absorption in ADMET (Absorption, Distribution, Metabolism, Excretion and Toxicity) prediction. While α-Amylase/α-Glucosidase-IN-10 acts as a substrate for P-gp and does not cross the blood-brain barrier (BBB), there may be a risk of central nervous system side effects[1].
  • HY-162396
    P-gp inhibitor 21 Inhibitor
    P-gp inhibitor 21 (Compound 56) is an inhibitor for P-glycoprotein (P-gp) transport, which reverses P-gp-mediated multidrug resistance (MDR) and exhibits antitumor efficacy in mice without significant cytotoxicity[1].
  • HY-126906
    Milbemycin A4 Inhibitor
    Milbemycin A4 inhibits P-glycoprotein activity, and reverses multidrug resistance of tumor cells. Milbemycins are a family of macrolide antibiotics with insecticidal and acaricidal activity[1]sup>[2].
  • HY-W854295
    Phosphatidylinositol-1,2-dioctanoyl sodium Inhibitor
    Phosphatidylinositol-1,2-dioctanoyl sodium significantly inhibits transmembrane P-gp transport in a reproducible, cell line-independent, and substrate-independent manner. Phosphatidylinositol-1,2-dioctanoyl sodium plays an important role in signal transduction and cell movement[1].
  • HY-135336BS
    (Rac)-Verapamil-d7 hydrochloride
    (Rac)-Verapamil-d7 (hydrochloride) is the deuterium labeled (Rac)-Verapamil[1].
  • HY-125486
    Reversin 121 Inhibitor 99.31%
    Reversin 121 is a P-glycoprotein inhibitor. Reversin 121 increases the ATPase activity of MDR1. Reversin 121 reverses P-glycoprotein-mediated multidrug resistance. Reversin 121 can be used in the research of cancers[1][2].
  • 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[1].
  • HY-11018S2
    Risperidone-d6 Inhibitor
    Risperidone-d6 (R 64 766-d6) is the deuterium labeled Risperidone (HY-11018). 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[1][2].
  • HY-15134
    ONT-093 99.21%
    ONT-093 is a potent inhibitor of P-glycoprotein pump. ONT-093 has the potential for the research cancer diseases[1].
  • HY-17411
    Limonin Inhibitor 98.68%
    Limonin inhibits HIV-1 with an EC50 of 60.0 μM. Limonin induces human colon adenocarcinoma cells apoptosis with an IC50 of 54.74 μM. Limonin has antiviral and antitumor activities[1][2][4].
  • HY-11018B
    Risperidone mesylate Inhibitor
    Risperidone mesylate(R 64 766 mesylate) 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-162040
    P-gp inhibitor 17 Inhibitor
    P-gp inhibitor 17 (compound 2g) is a P-gp inhibitor directly interacted with the transmembrane domain of P-gp. P-gp inhibitor 17 can be used for P-gp-mediated multidrug-resistant in tumor cells study[1].
  • HY-119101
    AZD-5672 Inhibitor
    AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 shows moderate activity against the hERG ion channel (binding IC50=7.3 μM). AZD5672 is a substrate of human P-gp, and inhibits P-gp-mediated digoxin transport (IC50=32 μM). AZD-5672 can be used for the research of rheumatoid arthritis[1][2][3].
  • HY-149981
    P-gp inhibitor 13 Inhibitor
    P-gp inhibitor 13 is a P-gp inhibitor. P-gp inhibitor 13 can reverse P-glycoprotein-mediated paclitaxel resistance in A2780/T cell. P-gp inhibitor 13 can be used for the research of advanced acute myeloid leukemia[1].
  • HY-U00247
    MCI826 Agonist
    MCI826 is a P-glycoprotein (P-gp) antagonist.