P-glycoprotein

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.

P-glycoprotein 相关产品(49)

  • GC33375 structure
    GC33375MCI826
    CAS: 140646-80-6

    MCI826是一种P-glycoprotein(P-gp)拮抗剂。

  • GC35692 structure
    GC35692Chrysosplenetin
    CAS: 603-56-5
    纯度: >99.50%

    A flavonoid with diverse biological activities

  • GC35727 structure
    GC35727Coniferyl ferulate
    CAS: 63644-62-2
    纯度: >98.50%

    A monolignal conjugate with diverse biological activities

  • GC35892 structure
    GC35892Dofequidar
    CAS: 129716-58-1

    A quinoline derivative and inhibitor of multidrug resistance

  • GC36034 structure
    GC36034FD 12-9
    CAS: 1451741-22-2

    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。

  • GC36345 structure
    GC36345Isosinensetin
    CAS: 17290-70-9
    纯度: >98.00%

    A polymethoxylated flavone with anticancer and anti-inflammatory activities

  • GC36855 structure
    GC36855Paris saponin VII
    CAS: 68124-04-9
    纯度: >98.00% / >98.50%

    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.

  • GC36891 structure
    GC36891P-gp modulator 1
    CAS: 2249749-39-9

    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。

  • GC37832 structure
    GC37832TTT-28
    CAS: 1609138-51-3

    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)。

  • GC39701 structure
    GC39701Convallatoxin
    CAS: 508-75-8
    纯度: >98.00%

    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。

  • GC45150 structure
    GC45150Voacamine
    CAS: 3371-85-5
    纯度: >98.00%

    An alkaloid with diverse biological activities

  • GC50254 structure
    GC50254Tariquidar dihydrochloride
    CAS: 1992047-62-7

    A P-glycoprotein inhibitor

  • GC60407 structure
    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。

  • GC60408 structure
    GC60408(R)-Verapamil hydrochloride
    CAS: 38176-02-2
    纯度: >98.50%

    (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。

  • GC61811 structure
    GC61811Verapamil
    CAS: 52-53-9
    纯度: >99.50%

    Verapamil是 L 型钙通道阻滞剂和肾上腺素能受体拮抗剂,常用于高血压、心律失常和心绞痛的研究。

  • GC63175 structure
    GC63175Roemerine
    CAS: 548-08-3

    An aporphine alkaloid with diverse biological activities

  • GC64274 structure
    GC64274AZD-5672
    CAS: 780750-65-4

    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。

  • GC65183 structure
    GC65183P-gp inhibitor 1
    CAS: 2050747-49-2
    纯度: >98.00%

    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。

  • GC65184 structure
    GC65184YS-370
    CAS: 2470908-79-1
    纯度: >98.00%

    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。

  • GC65385 structure
    GC65385Ganoderenic acid B
    CAS: 100665-41-6

    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。

  • GC67920 structure
    GC67920WS-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)。

  • GC71999 structure
    GC71999Boeravinone B
    CAS: 114567-34-9
    纯度: >97.00%

    Boeravinone B,金黄色葡萄球菌和人类P-糖蛋白的NorA细菌外排泵的双重抑制剂,可减少细菌的生物膜形成和细胞内侵袭。

  • GC73573 structure
    GC73573hCA/Wnt/β-catenin-IN-1
    CAS: 3032826-63-1
    纯度: >99.00%

    hCA/Wnt/β-catenin-IN-1 (Compd 15)是hCA的抑制剂(Ki: 33.6, 24.1, 6.8 nM对hCA II, hCA IX, hCA XII) hCA/Wnt/β-catenin-IN-1降低P-gp活性。

  • GN10020 structure
    GN10020Piperine
    CAS: 94-62-2
    纯度: >98.50% / >98.00%

    A natural alkaloid with diverse biological actions