2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. Tariquidar dihydrochloride

Tariquidar dihydrochloride  (Synonyms: XR9576 dihydrochloride)

Cat. No.: HY-110377
Handling Instructions Technical Support

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

For research use only. We do not sell to patients.

CAS No. : 1992047-62-7

Size Stock
50 mg   Get quote  
100 mg   Get quote  
250 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Other In-stock Forms of Tariquidar dihydrochloride:

Other Forms of Tariquidar dihydrochloride:

Tariquidar dihydrochloride Related Antibodies

Top Publications Citing Use of Products

56 Publications Citing Use of MCE Tariquidar dihydrochloride

In Vivo Efficacy Study
Cell Proliferation/Viability Assay
WB
Cell Imaging/Staining
Flow Cytometry

    Tariquidar dihydrochloride 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).

    Tariquidar dihydrochloride 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.

    Tariquidar dihydrochloride 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 dihydrochloride 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.

    Tariquidar dihydrochloride 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).

    • Biological Activity

    • Protocol

    • Purity & Documentation

    • References

    • Customer Review

    Description

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

    IC50 & Target

    Kd: 5.1 nM (P-gp)[1]
    In Vitro

    Tariquidar (XR9576) is a potent modulator of P-gp mediated [3H]-Vinblastine and [3H]-Paclitaxel transport as it increases the steady-state accumulation of these cytotoxics in CHrB30 cells to levels observed in non-P-gp-expressing AuxB1 cells (EC50=487±50 nM). [3H]-Tariquidar binds to CHrB30 membranes with the highest affinity (Kd=5.1±0.9 nM, n=7) and a binding capacity (Bmax) of 275±15 pmol/mg membrane protein. In contrast to the parental cell line, the accumulation of [3H]-Vinblastine is increased in a dose-dependent fashion by the modulators Tariquidar (EC50=487±50 nM). The MDR modulator Tariquidar is able to inhibit 60-70% of the vanadate-sensitive ATPase activity, with potent IC50 value of 43±9 nM[1]. Tariquidar (XR9576) potentiates the cytotoxicity of several drugs including Doxorubicin, Paclitaxel, Etoposide, and Vincristine; complete reversal of resistance is achieved in the presence of 25-80 nM XR9576. Tariquidar is a potent inhibitor of photoaffinity labeling of P-gp by [3H]Azidopine implying a direct interaction with the protein[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

    Tariquidar dihydrochloride Related Antibodies
    In Vivo

    In mice bearing the intrinsically resistant MC26 colon tumors, coadministration of Tariquidar (XR9576) potentiates the antitumor activity of Doxorubicin without a significant increase in toxicity; maximum potentiation is observed at 2.5-4.0 mg/kg dosed either i.v. or p.o. In addition, coadministration of Tariquidar (6-12 mg/kg p.o.) fully restores the antitumor activity of Paclitaxel, Etoposide, and Vincristine against two highly resistant MDR human tumor xenografts (2780AD, H69/LX4) in nude mice. Tariquidar is found to also significantly potentiate the antitumor activity of doxorubicin against s.c. MC26 tumors in vivo[2].

    MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
    Molecular Weight

    719.65

    Formula

    C38H40Cl2N4O6
    CAS No.
    SMILES

    [H]Cl.[H]Cl.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
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    Please store the product under the recommended conditions in the Certificate of Analysis.
    Purity & Documentation
    References
    Cell Assay
    [2]

    Cells (EMT6 AR1.0 8×102/well; A2780 5×103/well; 2780AD 6×103/well) are seeded into 96-well plates. After ~4 h, varying concentrations of Tariquidar are added, and cells are incubated for an additional 4 days (EMT6 AR1.0) or 6 days (2780AD) before quantification of cell growth and calculation of IC10 values (concentration resulting in 10% inhibition of cell growth)[2].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    Animal Administration
    [2]

    Mice[2]
    MC26 tumor slurry is implanted s.c. in BALB/c mice (day 0). The animals are then randomized, 24 h later, into groups of 15-18 and treated once with various regimens. Tariquidar or vehicle is administered either i.v. via a lateral tail vein or p.o. with Doxorubicin (5 mg/kg) or vehicle i.v. The modulator is administered either i.v. at 2-4 mg/kg (10 mL/kg) at the same time as Doxorubicin or p.o. at 2-8 mg/kg (10 mL/kg) 1 h before the Cytotoxic drug. GG918 is administered p.o. 1 h before doxorubicin. All of the animals are weighed twice weekly. The animals are killed by cervical dislocation on day 14, and the tumors are excised and weighed. The data are analyzed by Student’s t test.
    Rats[2]
    Male CD rats (3 animals per time point) are dosed i.v. with paclitaxel alone [15 min infusion at 10 mg/kg in Tween 80:ethanol:5% dextrose (5:10:85% v/v/v)] or in combination with Tariquidar (10 mg/kg). Tariquidar is administered as a bolus (i.v.) dose 15 min before infusion of Paclitaxel. Blood samples are collected by cardiac puncture using heparinized syringes at various times between 0.083 and 48 h and are centrifuged to prepare plasma, which is stored at −20°C until analysis. Paclitaxel concentration in plasma samples is measured by a LC-MS/MS assay.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.
    References
    • No file chosen (Maximum size is: 1024 Kb)
    • If you have published this work, please enter the PubMed ID.
    • Your name will appear on the site.

    Tariquidar dihydrochloride Related Classifications

    • Molarity Calculator

    • Dilution Calculator

    The molarity calculator equation

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    Mass   Concentration   Volume   Molecular Weight *
    = × ×

    The dilution calculator equation

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
    × = ×
    C1   V1   C2   V2
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

    Keywords:

    Tariquidar1992047-62-7XR9576XR 9576XR-9576P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

    Your Recently Viewed Products:

    Inquiry Online

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Requested Quantity *

    Applicant Name *

    		 

    Salutation

    Email Address *

    		 

    Phone Number *

    Department

    		 

    Organization Name *

    City

    State

    Country or Region *

    		      

    Remarks

    Bulk Inquiry

    Inquiry Information

    Product Name:
    Tariquidar dihydrochloride
    Cat. No.:
    HY-110377
    Quantity:
    MCE Japan Authorized Agent:

    Customer Review

    Thank You for Your Feedback!

    Request for HNMR Report

    Please fill out this form to request the QC report. We will send it to your Email address shortly.

    Your information is safe with us. * Required Fields.

    Product Name

    		  

    Lot #

    Applicant Name *

    		 

    Email Address *

    Phone Number

    		 

    Department *

    Organization Name *

    		 

    Country or Region *

    Remarks

    SAFETY DATA SHEET (SDS)

    Request for HNMR Report

    We have received your request and will respond to you as soon as possible.