P-gp

Inhibitory Selectivity

Catalog No.	Inhibitor Name	P-gp	Other
A10549	Zosuquidar 3HCl	**
A11584	Tariquidar	***
A12324	Elacridar (GF120918)		BCRP

Notes:
1.Hover mouse over " * " to view the IC50 value.(A few compounds have proven potency but without published IC50 data.)
2.For more details about the compound, click on the product name of your interest.
3.The higher the number of " * " is, the more potent the inhibitor or activator is.
4."" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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FD 12-9

Catalog No. A18393
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P-gp/BCRP dual 抑制剂

FD 12-9 is a flavonoid dimer, acts as a dual inhibitor of P-gp and BCRP, with EC50s of 285 nM and 0.9 nM, respectively. Anti-glioblastoma activity. 了解更多

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KS-176

Catalog No. A16195
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BCRP 抑制剂

KS-176是乳腺癌抗性蛋白（BCRP）多药转运蛋白的有效和选择性抑制剂（在Pheo A和Hoechst 33342分析中，IC50值分别为0.59和1.39 uM）。了解更多

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MC 70 HCl

Catalog No. A16080
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P-gp 抑制剂

MC 70 HCl是有效的P-gp抑制剂（EC50 = 0.69 uM）。了解更多

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Laniquidar

Catalog No. A13532
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P-gp 抑制剂

Laniquidar是第三代P-gp抑制剂，已在临床试验中用于调节多药耐药转运蛋白。了解更多

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ONT-093

Catalog No. A13531
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P-gp 抑制剂

ONT-093是口服可生物利用的P-糖蛋白泵抑制剂，可潜在逆转接受癌症化学疗法的患者的多药耐药性。了解更多

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XR9576

Catalog No. A13961
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P-glycoprotein 抑制剂

XR9576是一种 P-glycoprotein (P-gp) 抑制剂，Kd值为5.1 nM。正在研究中作为抗癌多药耐药性的佐剂。了解更多

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Tariquidar (XR9576)

Catalog No. A11584
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P-gp 抑制剂

Tariquidar (XR9576)是一种P-糖蛋白药物外排泵抑制剂。了解更多

Product Citations (4)

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- Yuko Sasaki, .et al. Intestinal Permeability of Drugs in Caco-2 Cells Cultured in Microfluidic Devices, Biol Pharm Bull, 2022, 45(9):1246-1253 PMID: 36047192
- Sugisawa N, .et al. Novel Potent ABCB1 Modulator, Phenethylisoquinoline Alkaloid, Reverses Multidrug Resistance in Cancer Cell, Mol Pharm, 2018, Sep 4;15(9):4021-4030 PMID: 30052463
- Samy A. F. Morad, .et al. Role of P-glycoprotein inhibitors in ceramide-based therapeutics for treatment of cancer, Biochem Pharmacol, 2017, Apr 15; 130: 21-33 PMID: 28189725
- Debora Petroni, .et al. Synthesis and In Vivo Imaging of N-(3-[11C]Methoxybenzyl)-2-(3-Methoxyphenyl)ethylaniline as a Potential Targeting Agent for P-glycoprotein, Mol Imaging Biol, 2016, Dec;18(6):916-923 PMID: 27234445
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Elacridar (GF120918)

Catalog No. A12324
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P-gp & BCRP 抑制剂

Elacridar (GF120918)是一种原型BCRP抑制剂，可抑制Bcrp1介导的转运。了解更多

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- Leo Shen, .et al. A forward genetic screen identifies modifiers of rocaglate responsiveness, Sci Rep, 2021, Sep 16;11(1):18516 PMID: 34531456
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PSC-833 (Valspodar)

Catalog No. A11080
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MDR1/P-gp 抑制剂

PSC-833 (Valspodar)是一种P-糖蛋白（P-gp）调节剂，可抑制P-gp介导的多药耐药性（MDR）。了解更多

Product Citations (5)

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- Somin Lee, .et al. BBB-on-a-Chip: Modeling Functional Human Blood-Brain Barrier by Mimicking 3D Brain Angiogenesis Using Microfluidic Chip, Methods Mol Biol, 2022, 2492:251-263 PMID: 35733049
- Somin Lee, .et al. 3D brain angiogenesis model to reconstitute functional human blood?Cbrain barrier in vitro, ?Biotechnol Bioeng, 2019, 10 November
- Somin Lee, .et al. 3D brain angiogenesis model to reconstitute maturation of functional human blood-brain barrier in vitro, bioRxiv, 2018, Nov. 18
- Watanabe N, .et al. The possible clinical impact of risperidone on P-glycoprotein-mediated transport of tacrolimus: A case report and in vitro study, Biopharm Drug Dispos, 2018, Jan;39(1):30-37 PMID: 29055041
- Higashi H, .et al. In Vitro P-Glycoprotein-Mediated Transport of Tadalafil: A Comparison with Sildenafil, Biol Pharm Bull, 2017, 40(8):1314-1319 PMID: 28769012
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Elacridar hydrochloride

Catalog No. A15077
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P-gp 抑制剂

Elacridar hydrochloride是一种P-糖蛋白抑制剂，已在体内和体外用作P-糖蛋白（Pgp）的工具抑制剂，以研究转运蛋白在处理各种测试分子中的作用。了解更多

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Zosuquidar

Catalog No. A15289
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P-gp 抑制剂

Zosuquidar是P-糖蛋白介导的多药耐药性的有效调节剂，Ki为60 nM。了解更多

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TTT-28

Catalog No. A13033
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ABCB1 (P-gp/MDR1) inhibitor

TTT-28 is a synthesized thiazole-valine peptidomimetic, a novel selective inhibitor of ABCB1 (P-gp/MDR1) with high efficacy and low toxicity. 了解更多

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Norverapamil hydrochloride

Catalog No. A12249
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P-gp inhibitor

Norverapamil hydrochloride ((??)-Norverapamil hydrochloride), an N-demethylated metabolite of Verapamil, is a L-type calcium channel blocker and a P-glycoprotein (P-gp) function inhibitor. 了解更多

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P-gp inhibitor 1

Catalog No. A13384
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P-gp inhibitor

P-gp inhibitor 1 is a novel inhibitor reversing P-glycoprotein-mediated multidrug resistance. 了解更多

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