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
- Cat.No. 产品名称 Information
- GC71999 Boeravinone B 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。
- 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)。
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GC65385
Ganoderenic acid B
灵芝烯酸 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。 - 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。
- 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。
- 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。
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GC63175
Roemerine
莲碱,(-)-Roemerine
An aporphine alkaloid with diverse biological activities -
GC61811
Verapamil
维拉帕米; (±)-Verapamil; CP-16533-1
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。 -
GC60408
(R)-Verapamil hydrochloride
R-维拉帕米,(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。 -
GC60407
(R)-Verapamil D7 hydrochloride
(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。 -
GC39701
Convallatoxin
铃兰毒苷
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。 -
GC50254
Tariquidar dihydrochloride
XR9576 dihydrochloride
A P-glycoprotein inhibitor - 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)。
- 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。
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GC36855
Paris saponin VII
重楼皂苷 VII; Chonglou 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. -
GC36345
Isosinensetin
异橙黄酮
A polymethoxylated flavone with anticancer and anti-inflammatory activities -
GC36034
FD 12-9
Ac12Az9
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。 -
GC35892
Dofequidar
1-[4-[2-羟基-3-(5-喹啉基氧基)丙基]-1-哌嗪基]-2,2-二苯基乙酮
A quinoline derivative and inhibitor of multidrug resistance -
GC35727
Coniferyl ferulate
阿魏酸松柏酯
A monolignal conjugate with diverse biological activities -
GC35692
Chrysosplenetin
猫眼草黄素
A flavonoid with diverse biological activities -
GC45150
Voacamine
老刺木胺
An alkaloid with diverse biological activities - GC33375 MCI826 MCI826是一种P-glycoprotein(P-gp)拮抗剂。
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GC33338
Biricodar (VX-710)
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。 -
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.
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GC33151
Polyoxyethylene stearate (POES)
聚氧乙烯硬脂酸酯; POES
聚氧乙烯硬脂酸酯(POES)(POES)是一种非离子型乳化剂。 -
GC32906
Sinapine
芥子碱
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. -
GC32593
Zamicastat (BIA 5-1058)
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。 -
GC32518
Norverapamil hydrochloride ((±)-Norverapamil hydrochloride)
盐酸去甲维拉帕米; (±)-Norverapamil hydrochloride; D591 hydrochloride
An L-type calcium channel blocker -
GC31340
Encequidar (HM30181)
HM30181; HM30181A
An inhibitor of P-glycoprotein -
GC30371
Alisol F
泽泻醇 F
A triterpene with anti-inflammatory and hepatoprotective activities -
GC30033
Sinapine thiocyanate
芥子碱硫氰酸盐
Sinapine thiocyanate is the thiocyanate salt form of Sinapine, which shows favorable biological activities such as antioxidant and radio-protective activities. - GC18470 NSC 23925 An inhibitor of P-gp
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GC18460
Roquefortine C
异烟棒曲霉素 C
A mycotoxin -
GC10391
Hypophyllanthin
(7S,8S,9R)-9-(3,4-二甲氧基苯基)-6,7,8,9-四氢-4-甲氧基-7,8-双(甲氧基甲基)萘并[1,2-D]-1,3-二恶茂,NSC 619044
A P-glycoprotein inhibitor -
GC12523
Reversan
CBLC4H10
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)。 -
GC13375
Dofequidar fumarate
MS-209
A quinoline derivative and inhibitor of multidrug resistance -
GC16609
LY335979 (Zosuquidar 3HCL)
唑喹达三盐酸盐; RS 33295-198 trihydrochloride; LY-335979 trihydrochloride
A modulator of P-gp -
GC12986
Risperidone
利培酮; R 64 766
An atypical antipsychotic -
GC16672
Zosuquidar
(2R)-1-{4-[(1AR,6R,10BS)-1,1-二氟-1,1A,6,10B-四氢二苯并[A,E]环丙并[C]环庚烯-6-基]哌嗪-1-基}-3-(喹啉-5-基氧基)丙-2-醇,LY335979;LY 335979;LY-335979
A modulator of P-gp -
GC16677
Valspodar
伐司扑达,PSC 833;PSC-833;PSC833
Valspodar 是一种有效的 P-糖蛋白 (P-gp) 抑制剂,广泛用于临床前和临床研究 。 -
GC10928
Tariquidar methanesulfonate, hydrate
TARIQUIDAR二甲磺酸盐六水合物,XR 9576;XR-9576;XR9576
A P-glycoprotein inhibitor -
GC17163
Elacridar hydrochloride
依克立达盐酸盐,GF 120918A;GF120918A;GF-120918A
An inhibitor of MRP-1 and BCRP -
GC17215
Elacridar
依克立达; GF120918; GW0918; GG918; GW120918
An inhibitor of MRP-1 and BCRP -
GC15570
Tariquidar
N-[2-[[4-[2-(6,7-二甲氧基-3,4-二氢-1H-异喹啉-2-基)乙基]苯基]氨基甲酰基]-4,5-二甲氧基苯基]喹啉-3-甲酰胺,XR9576, XR 9576, XR-9576,Tariquidar
A P-glycoprotein inhibitor -
GC10240
Atazanavir sulfate (BMS-232632-05)
硫酸阿扎那韦; BMS-232632 sulfate
An inhibitor of HIV-1 protease -
GC12945
Atazanavir
阿扎那韦; BMS-232632
An inhibitor of HIV-1 protease
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GN10020
Piperine
胡椒碱; Bioperine; 1-Piperoylpiperidine
A natural alkaloid with diverse biological actions -
GN10805
Protopanaxdiol
20 (S)-原人参二醇; 20-Epiprotopanaxadiol; 20(S)-APPD
A sapogenin with anticancer and antibacterial activities