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)
- GC35727Coniferyl ferulateCAS: 63644-62-2纯度: >98.50%
A monolignal conjugate with diverse biological activities
- GC36345IsosinensetinCAS: 17290-70-9纯度: >98.00%
A polymethoxylated flavone with anticancer and anti-inflammatory activities
- GC36855Paris saponin VIICAS: 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.
- GC36891P-gp modulator 1CAS: 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。
- GC39701ConvallatoxinCAS: 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。
- 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(R)-Verapamil hydrochlorideCAS: 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。
- GC65385Ganoderenic acid BCAS: 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。
- GC71999Boeravinone BCAS: 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。
- GC73573hCA/Wnt/β-catenin-IN-1CAS: 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。
| 货号 | 产品名称 | CAS号 | 纯度 | 结构 |
|---|---|---|---|---|
| GC33375 | MCI826 | 140646-80-6 | - | |
MCI826是一种P-glycoprotein(P-gp)拮抗剂。 | ||||
| GC35692 | Chrysosplenetin | 603-56-5 | >99.50% | |
A flavonoid with diverse biological activities | ||||
| GC35727 | Coniferyl ferulate | 63644-62-2 | >98.50% | |
A monolignal conjugate with diverse biological activities | ||||
| GC35892 | Dofequidar | 129716-58-1 | - | |
A quinoline derivative and inhibitor of multidrug resistance | ||||
| GC36034 | FD 12-9 | 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 | Isosinensetin | 17290-70-9 | >98.00% | |
A polymethoxylated flavone with anticancer and anti-inflammatory activities | ||||
| GC36855 | Paris saponin VII | 68124-04-9 | >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 | P-gp modulator 1 | 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 | TTT-28 | 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 | Convallatoxin | 508-75-8 | >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 | Voacamine | 3371-85-5 | >98.00% | |
An alkaloid with diverse biological activities | ||||
| GC50254 | Tariquidar dihydrochloride | 1992047-62-7 | - | |
A P-glycoprotein inhibitor | ||||
| 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 | (R)-Verapamil hydrochloride | 38176-02-2 | >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 | Verapamil | 52-53-9 | >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 | Roemerine | 548-08-3 | - | |
An aporphine alkaloid with diverse biological activities | ||||
| GC64274 | AZD-5672 | 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 | P-gp inhibitor 1 | 2050747-49-2 | >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 | YS-370 | 2470908-79-1 | >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 | Ganoderenic acid B | 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 | 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)。 | ||||
| GC71999 | Boeravinone B | 114567-34-9 | >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 | hCA/Wnt/β-catenin-IN-1 | 3032826-63-1 | >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 | Piperine | 94-62-2 | >98.50% / >98.00% | |
A natural alkaloid with diverse biological actions | ||||
