Tariquidar dimesylate
Based on 57 publication(s) in Google Scholar
Tariquidar dimesylate (XR9576 dimesylate) is a P-glycoprotein (P-gp) inhibitor. Tariquidar dimesylate increases the concentration of the drug in the brain by binding to P-glycoprotein, preventing it from transporting the drug from inside to outside the brain. Tariquidar dimesylate can be used in the study of blood-brain barrier penetration and multidrug resistance.
For research use only. We do not sell to patients.
- CAS No.: 625375-84-0
- Formula: C40H46N4O12S2
- Molecular Weight:838.94
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications Citing Use of MedChemExpress (MCE) Tariquidar dimesylate
More- Cell. 2023 Dec 7;186(25):5500-5516.e21. [Abstract]
- Cancer Res. 2026 May 27:10.1158/0008-5472.CAN-25-5172. [Abstract]
- Sci Bull. 2016 Apr;61(7):552-560.
- J Control Release. 2022 Sep:349:109-117. [Abstract]
- J Control Release. 2022 Feb:342:44-52. [Abstract]
- Small. 2020 Nov;16(44):e2004172. [Abstract]
- Cell Death Discov. 2021 Aug 5;7(1):204. [Abstract]
- Antioxidants (Basel). 2021 Jun 11;10(6):949. [Abstract]
- Phytother Res. 2026 Apr;40(4):1935-1950. [Abstract]
- Crit Rev Anal Chem. 2022;52(7):1557-1571. [Abstract]
- Commun Chem. 2024 Jul 13;7(1):158. [Abstract]
- Pharmaceutics. 2021 Feb 26;13(3):306. [Abstract]
- Eur J Med Chem. 2018 Mar 10:147:7-20. [Abstract]
- Eur J Med Chem. 2017 Feb 15:127:586-598. [Abstract]
- RSC Adv. 2016,6, 69083-69093.
- Hepatol Commun. 2024 May 2;8(5):e0437. [Abstract]
- Mar Drugs. 2024 Aug 30;22(9):396. [Abstract]
- Eur J Pharmacol. 2024 Apr 15:969:176431. [Abstract]
- Mar Drugs. 2023 Mar 14;21(3):178. [Abstract]
- Pharmaceuticals (Basel). 2023 Feb 24;16(3):349. [Abstract]
- Mar Drugs. 2023 Jan 14;21(1):54. [Abstract]
- Mar Drugs. 2022 Nov 25;20(12):738. [Abstract]
- Mar Drugs. 2022 Sep 23;20(10):597. [Abstract]
- Int J Mol Sci. 2026 Mar 11;27(6):2587. [Abstract]
- Int J Mol Sci. 2023 Mar 10;24(6):5298. [Abstract]
- Int J Mol Sci. 2022 Nov 29;23(23):14948. [Abstract]
- J Drug Deliv Sci Technol. May 2022, 103323.
- Eur J Pharm Sci. 2019 Jan 15:127:319-329. [Abstract]
- Sci Rep. 2022 Aug 9;12(1):13570. [Abstract]
- Mol Pharm. 2021 Jan 4;18(1):416-428. [Abstract]
- Mol Pharm. 2020 Sep 8;17(9):3477-3486. [Abstract]
- Mol Pharm. 2019 Mar 4;16(3):1282-1293. [Abstract]
- Sci Rep. 2017 Dec 22;7(1):18069. [Abstract]
- J Cereb Blood Flow Metab. 2021 Jul;41(7):1634-1646. [Abstract]
- J Cereb Blood Flow Metab. 2020 Jan;40(1):150-162. [Abstract]
- J Cereb Blood Flow Metab. 2016 Aug;36(8):1412-23. [Abstract]
- ACS Chem Neurosci. 2025 Sep 3;16(17):3340-3353. [Abstract]
- Langmuir. 2015 May 12;31(18):5115-22. [Abstract]
- Antiviral Res. 2021 Sep:193:105124. [Abstract]
- Antimicrob Agents Chemother. 2015 Nov 30;60(2):946-54. [Abstract]
- Pharm Res. 2017 Jan;34(1):148-160. [Abstract]
- J Nat Prod. 2022 Dec 23;85(12):2746-2752. [Abstract]
- J Nanopart Res. (2018) 20:176.
- Nucl Med Biol. 2018 May:60:29-36. [Abstract]
- PLoS One. 2026 Jan 21;21(1):e0341445. [Abstract]
- PLoS One. 2017 Sep 15;12(9):e0183662. [Abstract]
- Mol Imaging Biol. 2019 Apr;21(2):257-268. [Abstract]
- Eur J Drug Metab Pharmacokinet. 2018 Oct;43(5):599-606. [Abstract]
- Xenobiotica. 2020 Mar;50(3):354-362. [Abstract]
- bioRxiv. 2025 Sep 20.
- bioRxiv. 2025 Jun 24:2025.06.18.660465. [Abstract]
- Res Sq. 2025 May 16.
- Research Square Preprint. 2024 Feb 6.
- Research Square Print. 2022 Jul.
- RWTH Aachen University. 2021 Oct.
- Research Square Preprint. 2021 Mar.
- J Biomed Nanotechnol. 2018 Oct 1;14(10):1705-1718. [Abstract]
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In Vivo Efficacy Study
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Cell Proliferation/Viability Assay
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WB
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Flow Cytometry
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Cell Imaging/Staining
Biological Activity
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 625375-84-0
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Molecular Weight 838.94
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Formula C40H46N4O12S2
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SMILES
O=C(NC1=CC(OC)=C(C=C1C(NC2=CC=C(C=C2)CCN3CC4=C(CC3)C=C(C(OC)=C4)OC)=O)OC)C5=CC6=CC=CC=C6N=C5.OS(=O)(C)=O.OS(=O)(C)=O
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Synonyms
XR9576 dimesylate
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (57)
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Journal Impact Factor
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Most Recent
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Cell
2023 Dec 7;186(25):5500-5516.e21. PMID: 38016470
Tariquidar dimesylate purchased from MedChemExpress. Usage Cited in: Cell. 2023 Dec 7;186(25):5500-5516.e21. [Abstract]
Survival curves of mice under SD (SR means 48 h of recovery after SD) with i.p. administration of tariquidar (n = 5) or vehicle (n = 5).
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Cancer Res
Targeted KRASG12V Degradation in vivo Elicits Lung Adenocarcinoma Regression with Subsequent Relapse from Dysregulated Proteolysis. [Abstract]2026 May 27:10.1158/0008-5472.CAN-25-5172. PMID: 42200804 -
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J Control Release
2022 Sep:349:109-117. PMID: 35798092 -
J Control Release
2022 Feb:342:44-52. PMID: 34971693 -
Small
Active Transportation of Liposome Enhances Tumor Accumulation, Penetration, and Therapeutic Efficacy. [Abstract]2020 Nov;16(44):e2004172. PMID: 33030305
Tariquidar dimesylate purchased from MedChemExpress. Usage Cited in: Small. 2020 Nov;16(44):e2004172. [Abstract]
In vitro tumor penetration of the DOX-loaded liposomes in BxPC3 MTS. The BxPC3 MTS were prestained with or without a Pg-p inhibitor Tariquidar (10 nM) for 3 h. Subsequently, the MTS were cultured with DOX-loaded liposomes for 6 h. The MTS were visualized using CLSM in Z-stacks with 25 µm intervals. DOX (red).
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Cell Death Discov
Compound 968 reverses adriamycin resistance in breast cancer MCF-7ADR cells via inhibiting P-glycoprotein function independently of glutaminase. [Abstract]2021 Aug 5;7(1):204. PMID: 34354052
Tariquidar dimesylate purchased from MedChemExpress. Usage Cited in: Cell Death Discov. 2021 Aug 5;7(1):204. [Abstract]
MCF-7ADR cells were treated with ADR (2μM) alone or together with Tariquidar (TQ; 0.5 μM) for 48h. Cell viability was detected using the CCK8 assays.
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Antioxidants (Basel)
The Long-Term DEHP Exposure Confers Multidrug Resistance of Triple-Negative Breast Cancer Cells through ABC Transporters and Intracellular ROS. [Abstract]2021 Jun 11;10(6):949. PMID: 34208283
Tariquidar dimesylate purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2021 Jun 11;10(6):949. [Abstract]
Tariquidar (1.5 μM; 72 h). Western blotting results show the specific inhibition of both MRP1/ABCC1 and MDR1/ABCB1 after tariquidar treatment for 72 h in both control and DEHP-exposed MDA-MB-231 clones.
Tariquidar dimesylate purchased from MedChemExpress. Usage Cited in: Antioxidants (Basel). 2021 Jun 11;10(6):949. [Abstract]
Tariquidar (1.5 μM; 2 h). Enhanced Dox accumulation was observed following 2 h of Tariquidar pretreatment in DEHP-exposed MDA-MB-231 clones #1 and #2, analyzed by a BD Accuri TW C6 flow cytometer.
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Phytother Res
20(R)-Ginsenoside Rg3 Suppresses P-Glycoprotein-Mediated Multidrug Resistance in A549/Taxol Cells by Targeting MDM2-IκB-α Signaling Axis. [Abstract]2026 Apr;40(4):1935-1950. PMID: 41630373 -
Crit Rev Anal Chem
A Critical Review on Advancement in Analytical Strategies for the Quantification of Clinically Relevant Biological Transporters. [Abstract]2022;52(7):1557-1571. PMID: 33691566 -
Commun Chem
2024 Jul 13;7(1):158. PMID: 39003409 -
Pharmaceutics
Co-Delivery of Berberine Chloride and Tariquidar in Nanoliposomes Enhanced Intracellular Berberine Chloride in a Doxorubicin-Resistant K562 Cell Line Due to P-gp Overexpression. [Abstract]2021 Feb 26;13(3):306. PMID: 33652886 -
Eur J Med Chem
Design and synthesis of new potent N,N-bis(arylalkyl)piperazine derivatives as multidrug resistance (MDR) reversing agents. [Abstract]2018 Mar 10:147:7-20. PMID: 29421572 -
Eur J Med Chem
N-alkanol-N-cyclohexanol amine aryl esters: Multidrug resistance (MDR) reversing agents with high potency and efficacy. [Abstract]2017 Feb 15:127:586-598. PMID: 28113128 -
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Hepatol Commun
Inhibition of the transmembrane transporter ABCB1 overcomes resistance to doxorubicin in patient-derived organoid models of HCC. [Abstract]2024 May 2;8(5):e0437. PMID: 38696353 -
Mar Drugs
Stonikacidin A, an Antimicrobial 4-Bromopyrrole Alkaloid Containing L-Idonic Acid Core from the Northwestern Pacific Marine Sponge Lissodendoryx papillosa. [Abstract]2024 Aug 30;22(9):396. PMID: 39330277 -
Eur J Pharmacol
Suppression of hypoxia-induced CAV1 autophagic degradation enhances nanoalbumin-paclitaxel transcytosis and improves therapeutic activity in pancreatic cancer. [Abstract]2024 Apr 15:969:176431. PMID: 38395374 -
Mar Drugs
New Bioactive β-Resorcylic Acid Derivatives from the Alga-Derived Fungus Penicillium antarcticum KMM 4685. [Abstract]2023 Mar 14;21(3):178. PMID: 36976227 -
Pharmaceuticals (Basel)
Functionalized Lipid Nanocarriers for Simultaneous Delivery of Docetaxel and Tariquidar to Chemoresistant Cancer Cells. [Abstract]2023 Feb 24;16(3):349. PMID: 36986449 -
Mar Drugs
New Marine Fungal Deoxy-14,15-Dehydroisoaustamide Resensitizes Prostate Cancer Cells to Enzalutamide. [Abstract]2023 Jan 14;21(1):54. PMID: 36662227 -
Mar Drugs
New Guanidine Alkaloids Batzelladines O and P from the Marine Sponge Monanchora pulchra Induce Apoptosis and Autophagy in Prostate Cancer Cells. [Abstract]2022 Nov 25;20(12):738. PMID: 36547885 -
Mar Drugs
Cytotoxic N-Methylpretrichodermamide B Reveals Anticancer Activity and Inhibits P-Glycoprotein in Drug-Resistant Prostate Cancer Cells. [Abstract]2022 Sep 23;20(10):597. PMID: 36286421 -
Int J Mol Sci
2026 Mar 11;27(6):2587. PMID: 41898448 -
Int J Mol Sci
Identification and Empiric Evaluation of New Inhibitors of the Multidrug Transporter P-Glycoprotein (ABCB1). [Abstract]2023 Mar 10;24(6):5298. PMID: 36982374 -
Int J Mol Sci
Salvage Chemotherapy with Cisplatin, Ifosfamide, and Paclitaxel in Aggressive Variant of Metastatic Castration-Resistant Prostate Cancer. [Abstract]2022 Nov 29;23(23):14948. PMID: 36499277 -
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Eur J Pharm Sci
Population pharmacokinetic modeling to establish the role of P-glycoprotein on ciprofloxacin distribution to lung and prostate following intravenous and intratracheal administration to Wistar rats. [Abstract]2019 Jan 15:127:319-329. PMID: 30423435 -
Sci Rep
New diterpenes from the marine sponge Spongionella sp. overcome drug resistance in prostate cancer by inhibition of P-glycoprotein. [Abstract]2022 Aug 9;12(1):13570. PMID: 35945234 -
Mol Pharm
Pharmacokinetic Modeling of ( R)-[11C]verapamil to Measure the P-Glycoprotein Function in Nonhuman Primates. [Abstract]2021 Jan 4;18(1):416-428. PMID: 33315404 -
Mol Pharm
Pharmacokinetic Modeling of [18F]MC225 for Quantification of the P-Glycoprotein Function at the Blood-Brain Barrier in Non-Human Primates with PET. [Abstract]2020 Sep 8;17(9):3477-3486. PMID: 32787277 -
Mol Pharm
Inhibition of ABCB1 and ABCG2 at the Mouse Blood-Brain Barrier with Marketed Drugs To Improve Brain Delivery of the Model ABCB1/ABCG2 Substrate [11C]erlotinib. [Abstract]2019 Mar 4;16(3):1282-1293. PMID: 30694684 -
Sci Rep
LUCS (Light-Up Cell System), a universal high throughput assay for homeostasis evaluation in live cells. [Abstract]2017 Dec 22;7(1):18069. PMID: 29273711 -
J Cereb Blood Flow Metab
Complete inhibition of ABCB1 and ABCG2 at the blood-brain barrier by co-infusion of erlotinib and tariquidar to improve brain delivery of the model ABCB1/ABCG2 substrate [11C]erlotinib. [Abstract]2021 Jul;41(7):1634-1646. PMID: 33081568 -
J Cereb Blood Flow Metab
Age dependency of cerebral P-glycoprotein function in wild-type and APPPS1 mice measured with PET. [Abstract]2020 Jan;40(1):150-162. PMID: 30354871 -
J Cereb Blood Flow Metab
Regulation of P-glycoprotein expression in brain capillaries in Huntington's disease and its impact on brain availability of antipsychotic agents risperidone and paliperidone. [Abstract]2016 Aug;36(8):1412-23. PMID: 26661162 -
ACS Chem Neurosci
2025 Sep 3;16(17):3340-3353. PMID: 40815164 -
Langmuir
Self-assembled polymer/inorganic hybrid nanovesicles for multiple drug delivery to overcome drug resistance in cancer chemotherapy. [Abstract]2015 May 12;31(18):5115-22. PMID: 25927163 -
Antiviral Res
2021 Sep:193:105124. PMID: 34197862 -
Antimicrob Agents Chemother
Simultaneous Semimechanistic Population Analyses of Levofloxacin in Plasma, Lung, and Prostate To Describe the Influence of Efflux Transporters on Drug Distribution following Intravenous and Intratracheal Administration. [Abstract]2015 Nov 30;60(2):946-54. PMID: 26621623 -
Pharm Res
Tumor Targeting Synergistic Drug Delivery by Self-Assembled Hybrid Nanovesicles to Overcome Drug Resistance. [Abstract]2017 Jan;34(1):148-160. PMID: 27738951 -
J Nat Prod
Meroantarctines A-C, Meroterpenoids with Rearranged Skeletons from the Alga-Derived Fungus Penicillium antarcticum KMM 4685 with Potent p-Glycoprotein Inhibitory Activity. [Abstract]2022 Dec 23;85(12):2746-2752. PMID: 36413729 -
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Nucl Med Biol
A new method measuring the interaction of radiotracers with the human P-glycoprotein (P-gp) transporter. [Abstract]2018 May:60:29-36. PMID: 29529532 -
PLoS One
RIPK2 induces docetaxel resistance in prostate cancer through the NF-κB/P-gp signaling pathway. [Abstract]2026 Jan 21;21(1):e0341445. PMID: 41563982 -
PLoS One
Inflammatory cytokine production in tumor cells upon chemotherapy drug exposure or upon selection for drug resistance. [Abstract]2017 Sep 15;12(9):e0183662. PMID: 28915246 -
Mol Imaging Biol
SNAPshots of the MCHR1: a Comparison Between the PET-Tracers [18F]FE@SNAP and [11C]SNAP-7941. [Abstract]2019 Apr;21(2):257-268. PMID: 29948643 -
Eur J Drug Metab Pharmacokinet
Pharmacokinetics of the P-gp Inhibitor Tariquidar in Rats After Intravenous, Oral, and Intraperitoneal Administration. [Abstract]2018 Oct;43(5):599-606. PMID: 29616423 -
Xenobiotica
The potential role of human multidrug resistance protein 1 (MDR1) and multidrug resistance-associated protein 2 (MRP2) in the transport of Huperzine A in vitro. [Abstract]2020 Mar;50(3):354-362. PMID: 31132291 -
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bioRxiv
2025 Jun 24:2025.06.18.660465. PMID: 40666929 -
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J Biomed Nanotechnol
Folate-Targeted Redox-Responsive Polymersomes Loaded with Chemotherapeutic Drugs and Tariquidar to Overcome Drug Resistance. [Abstract]2018 Oct 1;14(10):1705-1718. PMID: 30041718
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)