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

P-glycoprotein

P-gp; Pgp; Multidrug resistance protein 1; MDR1; ATP-binding cassette sub-family B member 1; ABCB1; Cluster of differentiation 243; CD243

P-glycoprotein

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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.

Cat. No. Product Name Effect Purity Chemical Structure
  • HY-W009141
    1-Monopalmitin
    		Inhibitor 99.42%
    1-Monopalmitin, a bitter melon extract, inhibits the P-glycoprotein (P-gp) activity in intestinal Caco-2 cells.
    1-Monopalmitin
  • HY-D0194
    5(6)-Carboxy-2',7'-dichlorofluorescein
    		99.32%
    5(6)-Carboxy-2',7'-dichlorofluorescein is an ideal substrate for MRP2 vesicular transport assay, with excellent detection and transport properties.
    5(6)-Carboxy-2',7'-dichlorofluorescein
  • HY-N1941
    Isosinensetin
    		Inhibitor 99.90%
    Isosinensetin, a polymethoxylated flavone extracted from pericarpium citri reticulatae viride, exhibits inhibition on P-glycoprotein (P-gp) in MDR1-MDCKII cells.
    Isosinensetin
  • HY-106004
    Zamicastat
    		Inhibitor 99.93%
    Zamicastat (BIA 5-1058) is a dopamine β-hydroxylase (DBH) inhibitor and can cross the blood-brain barrier (BBB) to 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. Zamicastat reduces high blood pressure.
    Zamicastat
  • HY-N6932
    Voacamine
    		Inhibitor 99.64%
    Voacamine, an indole alkaloid, exhibits potent cannabinoid CB1 receptor antagonistic activity. Voacamine also inhibits P-glycoprotein (P-gp) action in multidrug-resistant tumor cells.
    Voacamine
  • HY-100750
    Norverapamil hydrochloride
    		Inhibitor 99.80%
    Norverapamil hydrochloride ((±)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
    Norverapamil hydrochloride
  • HY-N2453
    Convallatoxin
    		98.66%
    Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin ameliorates colitic inflammation via activation of PPARγ and suppression of NF-κB. Convallatoxin is a P-glycoprotein (P-gp) substrate and recognized Val982 as an important amino acid involved in its transport. Convallatoxin is an enhancer of ligand-induced MOR endocytosis with high potency and efficacy. Anti-inflammatory and anti-proliferative properties.
    Convallatoxin
  • HY-135336A
    (S)-Verapamil hydrochloride
    		98.30%
    (S)-Verapamil hydrochloride (S(-)-Verapamil hydrochloride) inhibits leukotriene C4 (LTC4) and calcein transport by MRP1. (S)-Verapamil hydrochloride leads to the death of potentially resistant tumor cells.
    (S)-Verapamil hydrochloride
  • HY-117452
    LY-402913
    		Inhibitor 99.86%
    LY-402913 is a selective multidrug resistance protein (MRP1) inhibitor.
    LY-402913
  • HY-135336
    (R)-Verapamil hydrochloride
    		Inhibitor 99.48%
    (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is an orally active P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport. (R)-Verapamil hydrochloride induces Apoptosis and inhibits L-type calcium channels BZPcc, DHPcc and PLLcc. (R)-Verapamil hydrochloride has anti-septic shock and anti-diabetic effects.
    (R)-Verapamil hydrochloride
  • HY-14942
    Berubicin
    		Inhibitor
    Berubicin (RTA 744 free base; WP 744) is a 4'-O-benzyldoxorubicin that inhibits P-gp and MRP1-mediated efflux and has anticancer activity. Berubicin inhibits glioblastoma multiforme (GBM) and exhibits cytotoxicity. Berubicin has poor bioavailability in mice.
    Berubicin
  • HY-101530
    Polyoxyethylene stearate
    Polyoxyethylene stearate (POES) is a non-ionic emulsifying agent.
    Polyoxyethylene stearate
  • HY-N2103
    Tenacissoside G
    		99.64%
    Tenacissoside G is a C21 steroid from the stems of Marsdenia tenacissima. Tenacissoside G reverses multidrug resistance in P-glycoprotein (Pgp)-overexpressing multidrug-resistant cancer cells.
    Tenacissoside G
  • HY-A0064S
    Verapamil-d3 hydrochloride
    		Inhibitor 99.57%
    Verapamil-d3 (hydrochloride) is the deuterium labeled Verapamil hydrochloride. 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].
    Verapamil-d<sub>3</sub> hydrochloride
  • HY-113805
    MC70
    		Inhibitor 99.50%
    MC70 is a potent and non-selective P-glycoprotein (P-gp) inhibitor with an EC50 of 0.69 µM. MC70 is an ABC transporters inhibitor and anticancer agent. MC70 interacts with ABCB1, ABCG2 and ABCC1.
    MC70
  • HY-15206S1
    Glyburide-d3
    		Inhibitor 99.24%
    Glyburide-d3 is the deuterium labeled Glibenclamide. 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].
    Glyburide-d<sub>3</sub>
  • HY-162753
    ZW-1226
    		Inhibitor 98.13%
    ZW-1226 is a selective inhibitor of MRP1, reducing the uptake activity of MRP1 vesicles by 65 % at 5 μM. ZW-1226 shows inhibition of MRP1 in a GSH dependent way and good selectivity for MRP1 over other major ABC transporters, including P-gp, BCRP, MRP2 and MRP3.
    ZW-1226
  • HY-N1457
    Chrysosplenetin
    		Inhibitor 99.68%
    Chrysosplenetin is one of the polymethoxylated flavonoids in Artemisia annua L. (Compositae) and other several Chinese herbs. Chrysosplenetin inhibits P-gp activity and reverses the up-regulated P-gp and MDR1 levels induced by artemisinin (ART). Chrysosplenetin significantly augments the rat plasma level and anti-malarial efficacy of ART, partially due to the uncompetitive inhibition effect of Chrysosplenetin on rat CYP3A.
    Chrysosplenetin
  • 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.
    Reversin 121
  • HY-119823
    PGP-4008
    		Inhibitor 99.69%
    PGP-4008 is a specific P-glycoprotein (Pgp) inhibitor. PGP-4008 inhibits tumor growth in a murine syngeneic Pgp-mediated multiple agent resistance (MDR) solid tumor model when given in combination with Doxorubicin.
    PGP-4008
Cat. No. Product Name / Synonyms Application Reactivity