Tariquidar

• UNSPSC Description:

  Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM)[1].

• Target Antigen:

  P-glycoprotein

• Type:

  Reference compound

• Related Pathways:

  Membrane Transporter/Ion Channel

• Applications:

  Cancer-programmed cell death

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/Tariquidar.html

• Purity:

  99.45

• Solubility:

  H2O : < 0.1 mg/mL

• Smiles:

  O=C(C1=CC2=CC=CC=C2N=C1)NC3=CC(OC)=C(OC)C=C3C(NC4=CC=C(CCN5CC6=C(C=C(OC)C(OC)=C6)CC5)C=C4)=O

• Molecular Weight:

  646.73

• References & Citations:

  [1]Martin C, et al. The molecular interaction of the high affinity reversal agent XR9576 with P-glycoprotein. Br J Pharmacol, 1999, 128(2), 403-411.|[2]Mistry P, et al. In vitro and in vivo reversal of P-glycoprotein-mediated multidrug resistance by a novel potent modulator, XR9576. Cancer Res, 2001, 61(2), 749-758.|[3]Zimmermann ES, et al. 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. Antimicrob Agents Chemother. 2015 Nov 30;60(2):946-54.|[4]Kao YH, et al. Regulation of P-glycoprotein expression in brain capillaries in Huntington's disease and its impact on brain availability of antipsychotic agents risperidone and paliperidone. J Cereb Blood Flow Metab. 2016 Aug;36(8):1412-23.|[5]Matzneller P, et al. Pharmacokinetics of the P-gp Inhibitor Tariquidar in Rats After Intravenous, Oral, and Intraperitoneal Administration. Eur J Drug Metab Pharmacokinet. 2018 Apr 3.Antimicrob Agents Chemother. 2015 Nov 30;60(2):946-54. |Antioxidants (Basel). 2021 Jun 11;10(6):949.|Antioxidants (Basel). 2024 Sep 1.|Antiviral Res. 2021 Jun 28;105124.|Cell Death Discov. 2021 Aug 5;7(1):204.|Cell. 2023 Dec 7;186(25):5500-5516.e21.|Commun Chem. 2024 Jul 13;7(1):158.|Crit Rev Anal Chem. 2021 Mar 10;1-15.|Eur J Drug Metab Pharmacokinet. 2018 Oct;43(5):599-606.|Eur J Med Chem. 2017 Feb 15;127:586-598. |Eur J Med Chem. 2018 Mar 10;147:7-20. |Eur J Pharm Sci. 2019 Jan 15;127:319-329.|Eur J Pharmacol. 2024 Feb 21:176431.|Hepatol Commun. 2024 May 2;8(5):e0437.|Int J Mol Sci. 2022, 23(23), 14948.|Int J Mol Sci. 2023 Mar 10.|J Biomed Nanotechnol. 2018 Oct 1;14(10):1705-1718.|J Cereb Blood Flow Metab. 2016 Aug;36(8):1412-23. |J Cereb Blood Flow Metab. 2021 Jul;41(7):1634-1646.|J Control Release. 2022 Jul 8;349:109-117.|J Drug Deliv Sci Technol. May 2022, 103323.|J Nanopart Res. (2018) 20:176.|J Nat Prod. 2022 Nov 22.|Langmuir. 2015 May 12;31(18):5115-22. |Mar Drugs. 2022, 20(10), 597.|Mar Drugs. 2022, 20(12), 738|Mar Drugs. 2023 Mar 14.|Mar Drugs. 2023, 21(1), 54.|Mar Drugs. 2024 Aug 30.|Mol Pharm. 2019 Mar 4;16(3):1282-1293. |Mol Pharm. 2021 Jan 4;18(1):416-428.|Pharm Res. 2017 Jan;34(1):148-160.|Pharmaceuticals. 2023 Feb 24; Feb 16(3), 349.|Pharmaceutics. 2021 Feb 26;13(3):306.|PLoS One. 2017 Sep 15;12(9):e0183662. |Research Square Preprint. 2021 Mar.|Research Square Preprint. 2024 Feb 6.|Research Square Print. 2022 Jul.|RSC Adv. 2016,6, 69083-69093.|Sci Bull. 2016 Apr;61(7):552-560.|Sci Rep. 2017 Dec 22;7(1):18069.|Sci Rep. 2022 Aug 9;12(1):13570.|Small. 2020 Nov;16(44):e2004172.|Xenobiotica. 2020 Mar;50(3):354-362. |J Cereb Blood Flow Metab. 2020 Jan;40(1):150-162.|Mol Imaging Biol. 2019 Apr;21(2):257-268. |Mol Pharm. 2020 Sep 8;17(9):3477-3486.|Nucl Med Biol. 2018 May;60:29-36. |RWTH Aachen University. 2021 Oct.|J Control Release. 2021 Dec 28;342:44-52.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Phase 3

• CAS Number:

  206873-63-4