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P-glycoprotein(P糖蛋白)

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.

Products for  P-glycoprotein

  1. Cat.No. 产品名称 Information
  2. GC67920 WS-898 WS-898 是一种高效的 ABCB1 抑制剂,能够逆转耐药SW620/Ad300、KB-C2 和 HEK293/ABCB1 细胞对紫杉醇(PTX)的耐药性(IC50 = 5.0、3.67 和 3.68 nM)。
  3. GC65385 Ganoderenic acid B Ganoderenic acid B 是从 Ganoderma lucidum 中分离的一种三萜类化合物。Ganoderenic acid B 可有效逆转 ABCB1 介导的HepG2/ADM 细胞对 Doxorubicin 的耐药性。
  4. GC65184 YS-370 YS-370 (compound 44) 是一种有效的、高选择性的、具有口服活性的 P-糖蛋白 (P-gp) 抑制剂。YS-370 刺激 P-gp ATPase 活性并对 CYP3A4 有中度抑制作用。YS-370 可有效逆转 SW620/AD300 和 HEK293T-ABCB1 细胞对紫杉醇和秋水仙碱的多药耐药性 (MDR)。YS-370 与紫杉醇联合使用具有更强的抗肿瘤活性。
  5. GC65183 P-gp inhibitor 1 P-gp inhibitor 1是一种新型的可逆转P-糖蛋白介导的多药耐药性抑制剂。
  6. GC64274 AZD-5672 AZD-5672 是一种口服有效的强效选择性 CCR5 拮抗剂 (IC50=0.32 nM)。AZD-5672 对 hERG 离子通道具有中等活性 (结合 IC50=7.3 μM)。AZD5672是人 P-gp 的底物,抑制 P-gp 介导的地高辛转运 (IC50=32 μM)。AZD-5672 可用于类风湿性关节炎的研究。
  7. GC63175 Roemerine An aporphine alkaloid with diverse biological activities
  8. GC61811 Verapamil Verapamil HCl (CP-16533-1,(±)-Verapamil hydrochloride) is an L-type calcium channel blocker that is a class IV anti-arrhythmia agent. Verapamil inhibits both permeability-glycoprotein (P-gp) and CYP3A4.
  9. GC60408 (R)-Verapamil hydrochloride (R)-Verapamilhydrochloride((R)-(+)-Verapamilhydrochloride)是一种P-糖蛋白(P-Glycoprotein)抑制剂。(R)-Verapamilhydrochloride抑制MRP1介导的转运,导致MRP1过表达细胞对抗癌药产生化学敏感性。
  10. GC60407 (R)-Verapamil D7 hydrochloride (R)-VerapamilD7hydrochloride((R)-(+)-VerapamilD7hydrochloride)是(R)-Verapamilhydrochloride的一种氘代化合物。(R)-Verapamilhydrochloride((R)-(+)-Verapamilhydrochloride)是一种P-糖蛋白抑制剂。(R)-Verapamilhydrochloride抑制MRP1介导的转运,导致MRP1过表达细胞对抗癌药产生化学敏感性。
  11. GC39701 Convallatoxin Convallatoxin 是从 Adonis amurensis Regel et Radde 分离得到的强心苷。Convallatoxin 通过激活 PPARγ 和抑制 NF-κB 改善结肠炎。Convallatoxin 是一种 P-糖蛋白 (P-gp) 底物,并识别 Val982 是参与其转运的重要氨基酸。Convallatoxin 是配体诱导的 MOR 胞吞作用的增强剂,具有很高的效力和功效。具有抗炎和抗增殖特性。
  12. GC50254 Tariquidar dihydrochloride A P-glycoprotein inhibitor
  13. GC37832 TTT-28 TTT-28 是一种噻唑-缬氨酸肽模拟物,高效 ABCB1 (P-gp/MDR1) 选择性抑制剂,低毒性。TTT-28 通过选择性阻断 ATP 结合盒亚家族 B 成员1 (ABCB1) 的外排功能, 逆转ABCB1介导的多药耐药性 (MDR)。
  14. GC36891 P-gp modulator 1 P-gp modulator 1 是一种高亲和力、口服有效的 p- 糖蛋白 (Pgp) 调节剂,可以逆转 Pgp 介导的多药抗性。
  15. GC36855 Paris saponin VII Chonglou Saponin VII (Dioscinin, Polyphyllin-VII, Paris saponin-VII), a kind of steroidal saponins from Chonglou (Rhizoma Paridis Chonglou), inhibits EMT and reduces the invasion of ovarian cancer cells via the GSK-3β/β-catenin signaling pathway.
  16. GC36345 Isosinensetin A polymethoxylated flavone with anticancer and anti-inflammatory activities
  17. GC36034 FD 12-9 FD 12-9 是一种类黄酮二聚体,为 P-gp 和 BCRP 的双重抑制剂,EC50 值分别为 285 nM 和 0.9 nM。具有抗胶质细胞瘤活性。
  18. GC35892 Dofequidar A quinoline derivative and inhibitor of multidrug resistance
  19. GC35727 Coniferyl ferulate A monolignal conjugate with diverse biological activities
  20. GC35692 Chrysosplenetin A flavonoid with diverse biological activities
  21. GC45150 Voacamine An alkaloid with diverse biological activities
  22. GC33375 MCI826 MCI826是一种P-glycoprotein(P-gp)拮抗剂。
  23. GC33338 Biricodar (VX-710) Biricodar (VX-710) (VX-710) 是 P-糖蛋白和 MRP-1 的调节剂;在多重耐药细胞中显示出有效的化学增敏活性。
  24. GC33185 Encequidar mesylate (HM30181 (mesylate)) HM30181 mesylate salt, a tetrazole derivative, is known as a P-glycoprotein inhibitor that has inhibitory activities on multidrug resistance in cancer cells[1,5].
  25. GC33151 Polyoxyethylene stearate (POES) 聚氧乙烯硬脂酸酯(POES)(POES)是一种非离子型乳化剂。
  26. GC32906 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.
  27. GC32593 Zamicastat (BIA 5-1058) Zamicastat (BIA 5-1058) (BIA 5-1058) 是一种多巴胺 β-羟化酶 (DBH) 抑制剂,可穿过血脑屏障 (BBB) 引起中枢和外周效应。
  28. GC32518 Norverapamil hydrochloride ((±)-Norverapamil hydrochloride) An L-type calcium channel blocker
  29. GC31340 Encequidar (HM30181) An inhibitor of P-glycoprotein
  30. GC30371 Alisol F A triterpene with anti-inflammatory and hepatoprotective activities
  31. GC30033 Sinapine thiocyanate Sinapine thiocyanate is the thiocyanate salt form of Sinapine, which shows favorable biological activities such as antioxidant and radio-protective activities.
  32. GC18470 NSC 23925 An inhibitor of P-gp
  33. GC18460 Roquefortine C A mycotoxin
  34. GC10391 Hypophyllanthin A P-glycoprotein inhibitor
  35. GC12523 Reversan MST-312 是一种端粒酶抑制剂。 MST-312 是绿茶表没食子儿茶素没食子酸酯 (EGCG) 的化学改性衍生物。 MST-312可用于癌症研究,例如多发性骨髓瘤(MM)。
  36. GC13375 Dofequidar fumarate A quinoline derivative and inhibitor of multidrug resistance
  37. GC16609 LY335979 (Zosuquidar 3HCL) A modulator of P-gp
  38. GC12986 Risperidone An atypical antipsychotic
  39. GC16672 Zosuquidar A modulator of P-gp
  40. GC16677 Valspodar A multidrug-resistance modulator
  41. GC10928 Tariquidar methanesulfonate, hydrate A P-glycoprotein inhibitor
  42. GC17163 Elacridar hydrochloride An inhibitor of MRP-1 and BCRP
  43. GC17215 Elacridar An inhibitor of MRP-1 and BCRP
  44. GC15570 Tariquidar A P-glycoprotein inhibitor
  45. GC10240 Atazanavir sulfate (BMS-232632-05) An inhibitor of HIV-1 protease
  46. GC12945 Atazanavir

    An inhibitor of HIV-1 protease

  47. GN10020 Piperine A natural alkaloid with diverse biological actions
  48. GN10805 Protopanaxdiol A sapogenin with anticancer and antibacterial activities

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