P-gp

P-gp製品

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  • P-gp阻害剤 (12)
  • P-gp作動薬(1)
  • P-gpモジュレータ(3)
  • 新製品
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S8028 Tariquidar Tariquidar is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM in CHrB30 cell line, reverses drug resistance in MDR cell Lines. Phase 3.
Drug Resist Updat, 2024, 73:101066
Nat Commun, 2023, 14(1):5035
Nat Commun, 2023, 14(1):5035
S1481 Zosuquidar 3HCl Zosuquidar 3HCl is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM in a cell-free assay. Phase 3.
Adv Healthc Mater, 2022, e2201984
Mol Cancer Ther, 2022, 21 (7): 1227–1235.
Mol Cancer Ther, 2022, molcanther.0013.2022
S4202 Verapamil HCl Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.
Cancers (Basel), 2023, 15(15)3774
EMBO Mol Med, 2022, 14(2):e14903
Cell Rep, 2022, 38(10):110468
S7772 Elacridar (GF120918) Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor.
Cancer Drug Resist, 2024, 7:3
bioRxiv, 2023, 10.1101/2023.05.18.539313
bioRxiv, 2023, 2023.05.18.539313
S7124 SC144 SC144 is the first-in-class orally active small-molecule gp130 inhibitor that induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes.
Nat Commun, 2024, 15(1):1041
Cell Stem Cell, 2023, 30(10):1382-1391.e5
Cells, 2022, 11(3)381
S4662 Atazanavir Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.
Int J Mol Sci, 2022, 23(23)15380
Chemistry, 2022, e202202798.
Sci Rep, 2021, 11(1):19443
S3600 Schisandrin B (Sch B) Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety.
Viruses, 2022, 14(2)353
Pharmacol Res, 2021, 166:105459
Ann Transl Med, 2021, 9(19):1500
S9145 Solamargine Solamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition.
Sci Rep, 2016, 6:36721
S3235 Sinapine Sinapine is an alkaloid isolated from seeds of the cruciferous species with antioxidant, antitumor and radio-protective activities. Sinapine inhibits the proliferation of Caco-2 cells via downregulation of P-glycoprotein.
Gene, 2022, 827:146460
S0921 Wilforine Wilforine (WR), a sesquiterpene pyridine alkaloid found in T. wilfordii plants, significantly inhibits the efflux activity of P-glycoprotein (P-gp).
S3431 Encequidar (HM30181) Encequidar (HM30181, HM30181A) is a potent and selective inhibitor of the adenosine triphosphate-binding cassette transporter P-glycoprotein (P-gp).
S4746 (20S)-Protopanaxadiol 20(S)-Protopanaxadiol (PPD, 20-Epiprotopanaxadiol), the main intestinal metabolite of ginsenosides, is one of the active ingredients in ginseng. 20(S)-Protopanaxadiol inhibits P-glycoprotein in multidrug resistant cancer cells.
E0080 UCLA GP130 2 UCLA GP130 2 (GP130 receptor agonist-1) is a potent, brain-penetrant and orally active Glycoprotein 130 (Gp130) receptor agonist, being a humanin mimetic binding to the GP130 D4-D5 domain and reducing NMDA-induced toxicity.
S9201 Levistilide A Levistilide A (Diligustilide), a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is a potential P-gp modulator and used for treating cancer.
S9563 Evodine Evodine, a natural product extracted from Evodiae fructus (EF), is a biomarker for quality assessment of EF in the Chinese Pharmacopoeia. Evodine is a potent P-gp inhibitor.
E1742New Reversan Reversan (CBLC4H10) is a selective and nontoxic inhibitor of multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (P-gp), with the potential to treat neuroblastoma and other MRP1-overexpressing drug-refractory tumors.
E0080 UCLA GP130 2 UCLA GP130 2 (GP130 receptor agonist-1) is a potent, brain-penetrant and orally active Glycoprotein 130 (Gp130) receptor agonist, being a humanin mimetic binding to the GP130 D4-D5 domain and reducing NMDA-induced toxicity.
S8028 Tariquidar Tariquidar is a potent and selective noncompetitive inhibitor of P-glycoprotein with Kd of 5.1 nM in CHrB30 cell line, reverses drug resistance in MDR cell Lines. Phase 3.
Drug Resist Updat, 2024, 73:101066
Nat Commun, 2023, 14(1):5035
Nat Commun, 2023, 14(1):5035
S4202 Verapamil HCl Verapamil HCl is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.
Cancers (Basel), 2023, 15(15)3774
EMBO Mol Med, 2022, 14(2):e14903
Cell Rep, 2022, 38(10):110468
S7772 Elacridar (GF120918) Elacridar (GF120918, GW120918, GG918, GW0918) is a potent P-gp (MDR-1) and BCRP inhibitor.
Cancer Drug Resist, 2024, 7:3
bioRxiv, 2023, 10.1101/2023.05.18.539313
bioRxiv, 2023, 2023.05.18.539313
S7124 SC144 SC144 is the first-in-class orally active small-molecule gp130 inhibitor that induces gp130 phosphorylation (S782) and deglycosylation, abrogates Stat3 phosphorylation and nuclear translocation, and further inhibits the expression of downstream target genes.
Nat Commun, 2024, 15(1):1041
Cell Stem Cell, 2023, 30(10):1382-1391.e5
Cells, 2022, 11(3)381
S3600 Schisandrin B (Sch B) Schisandrin B is the most abundant dibenzocyclooctadiene lignan present in the traditional Chinese medicinal herb Schisandra chinensis (Turcz.) Baill. It is a kind of ATR and P-gp inhibitor with high safety.
Viruses, 2022, 14(2)353
Pharmacol Res, 2021, 166:105459
Ann Transl Med, 2021, 9(19):1500
S9145 Solamargine Solamargine, a bioactive steroidal alkaloid isolated from Solanum aculeastrum, induces potent, non-selective cytotoxicity and P-gp inhibition.
Sci Rep, 2016, 6:36721
S3235 Sinapine Sinapine is an alkaloid isolated from seeds of the cruciferous species with antioxidant, antitumor and radio-protective activities. Sinapine inhibits the proliferation of Caco-2 cells via downregulation of P-glycoprotein.
Gene, 2022, 827:146460
S0921 Wilforine Wilforine (WR), a sesquiterpene pyridine alkaloid found in T. wilfordii plants, significantly inhibits the efflux activity of P-glycoprotein (P-gp).
S3431 Encequidar (HM30181) Encequidar (HM30181, HM30181A) is a potent and selective inhibitor of the adenosine triphosphate-binding cassette transporter P-glycoprotein (P-gp).
S4746 (20S)-Protopanaxadiol 20(S)-Protopanaxadiol (PPD, 20-Epiprotopanaxadiol), the main intestinal metabolite of ginsenosides, is one of the active ingredients in ginseng. 20(S)-Protopanaxadiol inhibits P-glycoprotein in multidrug resistant cancer cells.
S9563 Evodine Evodine, a natural product extracted from Evodiae fructus (EF), is a biomarker for quality assessment of EF in the Chinese Pharmacopoeia. Evodine is a potent P-gp inhibitor.
E1742New Reversan Reversan (CBLC4H10) is a selective and nontoxic inhibitor of multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (P-gp), with the potential to treat neuroblastoma and other MRP1-overexpressing drug-refractory tumors.
E0080 UCLA GP130 2 UCLA GP130 2 (GP130 receptor agonist-1) is a potent, brain-penetrant and orally active Glycoprotein 130 (Gp130) receptor agonist, being a humanin mimetic binding to the GP130 D4-D5 domain and reducing NMDA-induced toxicity.
S1481 Zosuquidar 3HCl Zosuquidar 3HCl is a potent modulator of P-glycoprotein-mediated multi-drug resistance with Ki of 60 nM in a cell-free assay. Phase 3.
Adv Healthc Mater, 2022, e2201984
Mol Cancer Ther, 2022, 21 (7): 1227–1235.
Mol Cancer Ther, 2022, molcanther.0013.2022
S4662 Atazanavir Atazanavir (Latazanavir, Zrivada, Reyataz, BMS-232632) is an azapeptide and HIV-protease inhibitor that is used in the treatment of HIV infections and AIDS in combination with other anti-HIV agents. Atazanavir is a substrate and inhibitor of cytochrome P450 isozyme 3A (CYP3A4) and an inhibitor and inducer of P-glycoprotein.
Int J Mol Sci, 2022, 23(23)15380
Chemistry, 2022, e202202798.
Sci Rep, 2021, 11(1):19443
S9201 Levistilide A Levistilide A (Diligustilide), a natural compound isolated from the traditional Chinese herb Ligusticum chuanxiong Hort, is a potential P-gp modulator and used for treating cancer.
E1742New Reversan Reversan (CBLC4H10) is a selective and nontoxic inhibitor of multidrug resistance-associated protein 1 (MRP1) and P-glycoprotein (P-gp), with the potential to treat neuroblastoma and other MRP1-overexpressing drug-refractory tumors.

P-gp阻害剤の選択性比較

P-gpシグナル伝達経路

P-gpシグナル伝達経路
Tags: P-gp inhibitor|P-gp agonist|P-gp activator|P-gp inducer|P-gp antagonist|P-gp signaling pathway|P-gp assay kit