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

Related Products

PDF 1.1 MB

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-181114
    P-gp-IN-34
    		Inhibitor
    P-gp-IN-34 (compound 4a) is an Mdr1p (Mdr1 pump) inhibitor. P-gp-IN-34 inhibits yeast to hyphal shift in Candida albicans. P-gp-IN-34 can be used for the research of candidiasis.
    P-gp-IN-34
  • HY-181404
    PA36-2
    		Inhibitor
    PA36-2 is an Mdr1 inhibitor and azole resistance reversal agent, with a IC50 of 1.0 μg/mL and a Kd of 4.209 μM against Candida albicans Mdr1. By effectively inhibiting the activity of the Mdr1 efflux pump, PA36-2 prevents the pumping of substrates out of cells, enhances the intracellular accumulation of azole antibiotics, and exerts a synergistic effect with antifungal agents such as Fluconazole (FLC) (HY-B0101). PA36-2 can be used in the research of azole-resistant candidiasis.
    PA36-2
  • HY-W699430
    Norverapamil-d6 hydrochloride
    		Inhibitor
    Norverapamil-d6 ((±)-Norverapamil-d6) hydrochloride is deuterium labeled Norverapamil (hydrochloride). 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-d<sub>6</sub> hydrochloride
  • HY-17367R
    Atazanavir (Standard)
    		Modulator
    Atazanavir (Standard) is the analytical standard of Atazanavir. This product is intended for research and analytical applications. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
    Atazanavir (Standard)
  • HY-16773
    Vedroprevir
    		Inhibitor
    Vedroprevir (GS-9451) is an inhibitor for HCV NS3/4A protease with an IC50 of 3.2 nM. Vedroprevir is also an inhibitor for breast cancer resistant protein (BCRP) with an IC50 of 1.4 μM. Vedroprevir inhibits P-gp, MRP1 and MRP2 with IC50 of 34, 14.9 and 12 μM, respectively. Vedroprevir exhibits good pharmacokinetic characteristics in rats and dogs.
    Vedroprevir
  • HY-50880R
    Elacridar hydrochloride (Standard)
    		Inhibitor
    Elacridar (hydrochloride) (Standard) is the analytical standard of Elacridar (hydrochloride). This product is intended for research and analytical applications. Elacridar hydrochloride (GF120918A) is an orally active P-glycoprotein (P-gp) and breast cancer resistance protein (BCRP) inhibitor. Elacridar hydrochloride can be used to examine the influence of efflux transporters on agent distribution to brain and it can be used for the research of cancer.
    Elacridar hydrochloride (Standard)
  • HY-13646AR
    Encequidar mesylate (Standard)
    		Inhibitor
    Encequidar (mesylate) (Standard) is the analytical standard of Encequidar (mesylate). This product is intended for research and analytical applications. Encequidar mesylate (HM30181 mesylate; HM30181A mesylate) is a competitive and potent P-glycoprotein inhibitor.
    Encequidar mesylate (Standard)
  • HY-N7305
    Jatrophane 5
    		Inhibitor
    Jatrophane 5 is a natural product of Jatropha carcas L. Jatrophane 5 has powerful inhibition of P-gp, higher than R(+)-verapamil (HY-14275) and Tariquidar (HY-10550) in colorectal multi-drug resistant cells (DLD1-TxR).
    Jatrophane 5
  • HY-120247
    TASP0434299
    		Ligand
    TASP0434299 (Compound 10) is a labeled ligand for the vasopressin V1b receptor. TASP0434299 exhibits high binding affinity for human and murine V1B receptors, with IC50 values of 0.526 nM and 0.641 nM, respectively, and shows potent antagonistic activity against the human V1B receptor with an IC50 of 0.639 nM. TASP0434299 is a substrate for human and rhesus monkey P-glycoprotein, resulting in low brain uptake in rhesus monkeys. TASP0434299 binds to V1B receptors in rat and monkey pituitary tissues in a saturable and specific manner both in vitro and in vivo. When radiolabeled with tritium or 11C, TASP0434299 serves as a prototype V1B receptor radiotracer to visualize V1B receptor in the pituitary gland of anesthetized monkeys via positron emission tomography.
    TASP0434299
  • HY-164683
    MRP1-IN-1
    		Inhibitor
    MRP1-IN-1 (Compound 9h) is a MRP1 inhibitor with an EC50 of 0.90 μM in HeLa-T5 cells.
    MRP1-IN-1
  • HY-123934
    VU6007477
    		Modulator
    VU6007477 is a brain-penetrant, selective M1 positive allosteric modulator (PAM) with an EC50 value of 230 nM. VU6007477 is also a human P-glycoprotein (P-gp) substrate with moderate permeability. VU6007477 displays improved central nervous system (CNS) penetration over the hydroxylated congeners. VU6007477 a pyranyl amide derivative, which is promising for research of robust cholinergic seizure activity.
    VU6007477
  • HY-10550AR
    Tariquidar methanesulfonate, hydrate (Standard)
    		Inhibitor
    Tariquidar (methanesulfonate, hydrate) (Standard) is the analytical standard of Tariquidar (methanesulfonate, hydrate). This product is intended for research and analytical applications. Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM.
    Tariquidar methanesulfonate, hydrate (Standard)
  • HY-135328
    Norverapamil
    		Inhibitor
    Norverapamil ((±)-Norverapamil), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor.
    Norverapamil
  • HY-17367S5
    Atazanavir-d24
    		Modulator
    Atazanavir-d24 (BMS-232632-d24) is deuterium labeled Atazanavir. Atazanavir (BMS-232632) is a highly selective and orally active HIV-1 protease inhibitor . Atazanavir is a substrate and inhibitor of CYP3A4, and an inhibitor of P-glycoprotein (P-gp). Atazanavir is also a SARS-CoV 3CLpro inhibitor with an IC50 of 3.49 μM. Atazanavir inhibits cardiac fibrosis, hyperlipidemia and induces malignant glioma death.
    Atazanavir-d<sub>24</sub>
  • HY-129698
    MS-073
    		Inhibitor
    MS-073 (CP162398) is a P-glycoprotein (P-gp) inhibitor. MS-073 reverses multidrug resistance in drug-resistant cells by competitively inhibiting drug binding to P-glycoprotein.
    MS-073
  • HY-U00247
    MCI826
    		Agonist
    MCI826 is a P-glycoprotein (P-gp) antagonist.
    MCI826
Cat. No. Product Name / Synonyms Application Reactivity