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抑制剂 & 化合物

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Cat. No.	Product Name	Target	Signaling Pathways
T63608	P-gp inhibitor 5
	P-gp inhibitor 5 是 P 糖蛋白 (P-gp) 的有效抑制剂，在 1.25 μM 和 2.5 μM 时 P-gp 抑制倍数分别为 2.5 和 3.0。P-gp inhibitor 5 对某些癌细胞表现出抗增殖效果。P-gp inhibitor 5 能够恢复细胞对 Vincristine 和 Paclitaxel 的敏感性，进而逆转 ABCB1/Flp-InTM-293 和 KBvin 的多药耐药 (MDR) 表型。
T13383	Zamicastat BIA 5-1058	BCRP; Hydroxylase; P-gp	Membrane transporter/Ion channel; Metabolism; Neuroscience
	Zamicastat (BIA 5-1058) 是多巴胺 β-羟化酶 (DBH) 抑制剂，可透过血脑屏障引起中枢和周边效应，具有降血压作用。它也是一种浓度依赖性的双重 P-gp 和 BCRP 抑制剂，IC50值分别为 73.8 和 17.0 μM。
T61501	Topoisomerase I inhibitor 5
	Topoisomerase I inhibitor 5 is an efficient inhibitor of topoisomerase I, with an IC50 value. It effectively disrupts DNA and inhibits the activity of topoisomerase I. Moreover, it can induce apoptosis in MCF-7 cells and arrest the cell cycle at the G1 phase. Topoisomerase I inhibitor 5 also exhibits potency in reversing P-gp-mediated resistance to Adriamycin [1].
T10453	BACE1-IN-5	Beta Amyloid; BACE	Neuroscience
	BACE1-IN-5 (Compound 15) 是一种 BACE1抑制剂，IC50为 9.1 nM。BACE1-IN-5还可抑制细胞 Aβ，IC50为 0.82 nM。并且，BACE1-IN-5 具有改善 hERG 抑制和 P-gp 外排的药物化学作用。
T83892	33-BCRP Inhibitor 33-Breast Cancer Resistance Protein Inhibitor
	33-BCRP抑制剂是一种乳腺癌耐药蛋白(BCRP)的抑制剂。它使得对米托蒽醌耐药的H460/MX20肺癌细胞对米托蒽醌诱导的细胞死亡更加敏感，无论是单独使用还是与UV辐射联合使用。33-BCRP抑制剂还能够增强表达P-糖蛋白(P-gp，亦称为多药耐药蛋白MDR)的KB-C2表皮癌细胞对秋水仙碱诱导的细胞死亡的敏感性。当使用5 µM浓度时，它能增加米托蒽醌在H460/MX20细胞中的细胞内积累。

化合物

Synonym: BIA 5-1058

Target: BCRP, Hydroxylase, P-gp

Topoisomerase I inhibitor 5

Target: Beta Amyloid, BACE

33-BCRP Inhibitor

Cat.No: T83892

Synonym: 33-Breast Cancer Resistance Protein Inhibitor

Target:

Cat. No.	Product Name	Target	Signaling Pathways
T37810	6',7'-Epoxybergamottin
	6'7'-Epoxybergamottin is a furanocoumarin found in grapefruit. It is a potent inhibitor of the cytochrome P450 (CYP) isoform CYP3A4 with an IC50 value of 0.30 ppm in a cell-free assay, 0.33 μM in HL7 human liver cells, and 0.22 μM in S9 human intestine cells. It has been studied in the context of drug interactions with grapefruit constituents. It is found in grapefruit juice at concentrations of 0.1-7.4 μM and inhibits the transport of talinolol , a permeability glycoprotein (P-gp/ABCB1) transpo...