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Home >> Signaling Pathways >> Membrane Transporter/Ion Channel >> 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.

Targets for  P-glycoprotein

Products for  P-glycoprotein

  1. Cat.No. Product Name Information
  2. GC60407 (R)-Verapamil D7 hydrochloride

    (R)-(+)-Verapamil D7 hydrochloride

     (R)-Verapamil D7 hydrochloride ((R)-(+)-Verapamil D7 hydrochloride) is a deuterium labeled (R)-Verapamil hydrochloride. (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs. (R)-Verapamil D7 hydrochloride Chemical Structure
  3. GC60408 (R)-Verapamil hydrochloride (R)-Verapamil hydrochloride ((R)-(+)-Verapamil hydrochloride) is a P-Glycoprotein inhibitor. (R)-Verapamil hydrochloride blocks MRP1 mediated transport, resulting in chemosensitization of MRP1-overexpressing cells to anticancer drugs. (R)-Verapamil hydrochloride Chemical Structure
  4. GC30371 Alisol F Alisol F is a triterpene isolated from Alisma orientalis, has immunosuppressive and anti-virus functions. Alisol F Chemical Structure
  5. GC12945 Atazanavir

    BMS 232632, CGP 73547

     An inhibitor of HIV-1 protease Atazanavir Chemical Structure
  6. GC10240 Atazanavir sulfate (BMS-232632-05) An inhibitor of HIV-1 protease Atazanavir sulfate (BMS-232632-05) Chemical Structure
  7. GC64274 AZD-5672 AZD-5672 is an orally active, potent, and selective CCR5 antagonist (IC50=0.32 nM). AZD-5672 Chemical Structure
  8. GC33338 Biricodar (VX-710)

    VX-710

     Biricodar (VX-710) (VX-710) is a modulator of P-glycoprotein and MRP-1; shows effective chemosensitizing activity in multidrug resistant cells. Biricodar (VX-710) Chemical Structure
  9. GC71999 Boeravinone B 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 Chemical Structure
  10. GC35692 Chrysosplenetin

    Chrysosplenol B, Chrysosptertin B, EMD 20940, Polycladin

     A flavonoid with diverse biological activities Chrysosplenetin Chemical Structure
  11. GC35727 Coniferyl ferulate

    A monolignal conjugate with diverse biological activities

     Coniferyl ferulate Chemical Structure
  12. GC39701 Convallatoxin Convallatoxin is a cardiac glycoside isolated from Adonis amurensis Regel et Radde. Convallatoxin Chemical Structure
  13. GC35892 Dofequidar A quinoline derivative and inhibitor of multidrug resistance Dofequidar Chemical Structure
  14. GC13375 Dofequidar fumarate

    MS-209

     MDR reversal agent Dofequidar fumarate Chemical Structure
  15. GC17215 Elacridar

    GF120918, GG918, GW0918

     An inhibitor of MRP-1 and BCRP Elacridar Chemical Structure
  16. GC17163 Elacridar hydrochloride An inhibitor of MRP-1 and BCRP Elacridar hydrochloride Chemical Structure
  17. GC31340 Encequidar (HM30181)

    Encequidar

     Encequidar (HM30181) (HM30181; HM30181A) is a potent and selective inhibitor of P-glycoprotein. Encequidar (HM30181) Chemical Structure
  18. GC33185 Encequidar mesylate (HM30181 (mesylate))

    HM30181 mesylate; HM30181A mesylate

     HM30181 mesylate salt, a tetrazole derivative, is known as a P-glycoprotein inhibitor that has inhibitory activities on multidrug resistance in cancer cells. Encequidar mesylate (HM30181 (mesylate)) Chemical Structure
  19. GC36034 FD 12-9

    Ac12Az9

     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. FD 12-9 Chemical Structure
  20. GC65385 Ganoderenic acid B Ganoderenic acid B is a lanostane-type triterpene isolated from Ganoderma lucidum. Ganoderenic acid B exhibits potent reversal effect on ABCB1-mediated multidrug resistance of HepG2/ADM cells to Doxorubicin. Ganoderenic acid B Chemical Structure
  21. GC73573 hCA/Wnt/β-catenin-IN-1

    hCA/Wnt/β-catenin-IN-1 (Compd 15) is an inhibitor of hCA (Ki: 33.6, 24.1, 6.8 nM for hCA II, hCA IX, hCA XII). hCA/Wnt/β-catenin-IN-1 reduces P-gp activity.

     hCA/Wnt/β-catenin-IN-1 Chemical Structure
  22. GC10391 Hypophyllanthin

    NSC 619044

     P-glycoprotein (P-gp) inhibitor Hypophyllanthin Chemical Structure
  23. GC36345 Isosinensetin

    6-Demethoxynobiletin

     Isosinensetin, a polymethoxylated flavone extracted from pericarpium citri reticulatae viride, exhibits inhibition on P-glycoprotein (P-gp) in MDR1-MDCKII cells. Isosinensetin Chemical Structure
  24. GC16609 LY335979 (Zosuquidar 3HCL)

    RS 33295-198; Zosuquidar trihydrochloride; LY335979; LY-335979

     Zosuquidar (LY335979) trihydrochloride is a P-glycoprotein (P-gp) inhibitor (Ki=59 nM). LY335979 (Zosuquidar 3HCL) shows anti-tumor activities, and can be used in acute myelogenous leukemia (AML) research. LY335979 (Zosuquidar 3HCL) Chemical Structure
  25. GC33375 MCI826 MCI826 is a P-glycoprotein (P-gp) antagonist. MCI826 Chemical Structure
  26. GC32518 Norverapamil hydrochloride ((±)-Norverapamil hydrochloride)

    D 591

     Norverapamil hydrochloride ((±)-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 hydrochloride ((±)-Norverapamil hydrochloride) Chemical Structure
  27. GC18470 NSC 23925 An inhibitor of P-gp NSC 23925 Chemical Structure
  28. GC65183 P-gp inhibitor 1 P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance. P-gp inhibitor 1 Chemical Structure
  29. GC36891 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). P-gp modulator 1 Chemical Structure
  30. GC36855 Paris saponin VII Paris saponin VII (Chonglou Saponin VII) is a steroidal saponin isolated from the roots and rhizomes of Trillium tschonoskii Maxim. Paris saponin VII-induced apoptosis in K562/ADR cells is associated with Akt/MAPK and the inhibition of P-gp. Paris saponin VII attenuates mitochondrial membrane potential, increases the expression of apoptosis-related proteins, such as Bax and cytochrome c, and decreases the protein expression levels of Bcl-2, caspase-9, caspase-3, PARP-1, and p-Akt. Paris saponin VII induces a robust autophagy in K562/ADR cells and provides a biochemical basis in the treatment of leukemia. Paris saponin VII Chemical Structure
  31. GN10020 Piperine

    Bioperine, NSC 21727, NPiperoylpiperidin

     Piperine Chemical Structure
  32. GC33151 Polyoxyethylene stearate (POES) Polyoxyethylene stearate (POES) (POES) is a non-ionic emulsifying agent. Polyoxyethylene stearate (POES) Chemical Structure
  33. GN10805 Protopanaxdiol

    20(S)-APPD, 20-Epiprotopanaxadiol

     Protopanaxdiol Chemical Structure
  34. GC12523 Reversan

    CBLC4H10

     inhibitor of multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (P-gp) Reversan Chemical Structure
  35. GC12986 Risperidone

    Apexidone, Psychodal, R 64766

    SR-2A inhibitor

     Risperidone Chemical Structure
  36. GC63175 Roemerine

    (-)-Roemerine, (R)-Roemerine

     Roemerine, an aporphine alkaloid, isolated from the leaves of Annona senegalensis, functions by interacting with P-glycoprotein. Roemerine reverses the multidrug-resistance phenotype with cultured cells. Roemerine Chemical Structure
  37. GC18460 Roquefortine C

    NSC 292134

     Roquefortine C is a mycotoxin that was first isolated from a strain of P. Roquefortine C Chemical Structure
  38. GC32906 Sinapine Sinapine is an alkaloid isolated from seeds of the cruciferous species. Sinapine Chemical Structure
  39. GC30033 Sinapine thiocyanate 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. Sinapine thiocyanate Chemical Structure
  40. GC15570 Tariquidar

    XR9576

     A P-glycoprotein inhibitor Tariquidar Chemical Structure
  41. GC50254 Tariquidar dihydrochloride

    XR9576 dihydrochloride

     Potent P-glycoprotein (P-gp) inhibitor Tariquidar dihydrochloride Chemical Structure
  42. GC10928 Tariquidar methanesulfonate, hydrate A P-glycoprotein inhibitor Tariquidar methanesulfonate, hydrate Chemical Structure
  43. GC37832 TTT-28 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. TTT-28 Chemical Structure
  44. GC16677 Valspodar

    Valspodar

     Valspodar is a potent inhibitor of P-glycoprotein (P-gp) widely used in preclinical and clinical studies [1]. Valspodar Chemical Structure
  45. GC61811 Verapamil Verapamil is an L-type calcium channel blocker and adrenergic receptor antagonist commonly used in studies of hypertension, arrhythmias and angina pectoris. Verapamil Chemical Structure
  46. GC45150 Voacamine

    NSC 82591

     Voacamine is an alkaloid originally isolated from Voacanga that has diverse biological activities. Voacamine Chemical Structure
  47. GC67920 WS-898 WS-898 Chemical Structure
  48. GC65184 YS-370 YS-370 (compound 44) is a potent, high selective, and orally active inhibitor of P-glycoprotein (P-gp). YS-370 stimulates the P-gp ATPase activity and has moderate inhibition against CYP3A4. YS-370 effectively reverses multidrug resistance (MDR) to paclitaxel and colchicine in SW620/AD300 and HEK293T-ABCB1 cells. YS-370 in combination with paclitaxel achieves much stronger antitumor activity. YS-370 Chemical Structure
  49. GC32593 Zamicastat (BIA 5-1058)

    BIA 5-1058

     Zamicastat (BIA 5-1058) (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 (BIA 5-1058) Chemical Structure
  50. GC16672 Zosuquidar A modulator of P-gp Zosuquidar Chemical Structure

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