2. Membrane Transporter/Ion Channel
  3. P-glycoprotein
  4. Tariquidar methanesulfonate, hydrate

Tariquidar methanesulfonate, hydrate  (Synonyms: XR9576 methanesulfonate, hydrate)

Cat. No.: HY-10550A Purity: 98.52%
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Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM.

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

CAS No. : 625375-83-9

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10 mM * 1 mL in DMSO
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Customer Review

Based on 56 publication(s) in Google Scholar

Other Forms of Tariquidar methanesulfonate, hydrate:

Tariquidar methanesulfonate, hydrate Related Antibodies

Top Publications Citing Use of Products

56 Publications Citing Use of MCE Tariquidar methanesulfonate, hydrate

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

    Tariquidar methanesulfonate, hydrate 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 methanesulfonate, hydrate 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 methanesulfonate, hydrate 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 methanesulfonate, hydrate 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 methanesulfonate, hydrate 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 methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) is a potent and specific inhibitor of P-glycoprotein (P-gp) with a Kd of 5.1 nM.

    IC50 & Target

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

    Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) 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 XR9576 (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 Tariquidar. 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 methanesulfonate, hydrate Related Antibodies
    In Vivo

    In mice bearing the intrinsically resistant MC26 colon tumors, coadministration of Tariquidar methanesulfonate, hydrate (XR9576 methanesulfonate, hydrate) 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

    892.99

    Formula

    C40H52N4O15S2
    CAS No.
    Appearance

    Solid

    Color

    Yellow to orange

    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.CS(=O)(O)=O.CS(=O)(O)=O.O.O.O
    Shipping

    Room temperature in continental US; may vary elsewhere.
    Storage

    4°C, sealed storage, away from moisture

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    Solvent & Solubility
    In Vitro: 

    DMSO : 100 mg/mL (111.98 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

    H2O : 5 mg/mL (5.60 mM; Need ultrasonic)

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.1198 mL 5.5992 mL 11.1983 mL
    5 mM 0.2240 mL 1.1198 mL 2.2397 mL
    View the Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

    • Molarity Calculator

    • Dilution Calculator

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

    Mass
    =
    Concentration
    ×
    Volume
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    Molecular Weight *

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

    This equation is commonly abbreviated as: C1V1 = C2V2

    Concentration (start)

    C1

    ×
    Volume (start)

    V1

    =
    Concentration (final)

    C2

    ×
    Volume (final)

    V2

    In Vivo:

    Select the appropriate dissolution method based on your experimental animal and administration route.

    For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
    To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
    The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

    • Protocol 1

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 5 mg/mL (5.60 mM); Clear solution

      This protocol yields a clear solution of ≥ 5 mg/mL (saturation unknown).

      Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

      Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
    In Vivo Dissolution Calculator
    Please enter the basic information of animal experiments:

    Dosage

    mg/kg

    Animal weight
    (per animal)

    g

    Dosing volume
    (per animal)

    μL

    Number of animals

    Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
    Please enter your animal formula composition:
    %
    DMSO +
    % 
    +
    %
    Tween-80 +
    %
    Saline
    Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
    The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
    Calculation results:
    Working solution concentration: mg/mL
    Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).

    *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

    The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
    Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
     If the continuous dosing period exceeds half a month, please choose this protocol carefully.
    Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
    Purity & Documentation

    Purity: 98.52%

    SDS (252 KB)

    COA (256 KB) LCMS (95 KB)

    Handling Instructions (2659 KB)
    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 methanesulfonate 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.
    Rat[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 methanesulfonate (10 mg/kg). Tariquidar methanesulfonate 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

    Complete Stock Solution Preparation Table

    * Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
    Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

    Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
    H2O / DMSO 1 mM 1.1198 mL 5.5992 mL 11.1983 mL 27.9958 mL
    5 mM 0.2240 mL 1.1198 mL 2.2397 mL 5.5992 mL
    DMSO 10 mM 0.1120 mL 0.5599 mL 1.1198 mL 2.7996 mL
    15 mM 0.0747 mL 0.3733 mL 0.7466 mL 1.8664 mL
    20 mM 0.0560 mL 0.2800 mL 0.5599 mL 1.3998 mL
    25 mM 0.0448 mL 0.2240 mL 0.4479 mL 1.1198 mL
    30 mM 0.0373 mL 0.1866 mL 0.3733 mL 0.9332 mL
    40 mM 0.0280 mL 0.1400 mL 0.2800 mL 0.6999 mL
    50 mM 0.0224 mL 0.1120 mL 0.2240 mL 0.5599 mL
    60 mM 0.0187 mL 0.0933 mL 0.1866 mL 0.4666 mL
    80 mM 0.0140 mL 0.0700 mL 0.1400 mL 0.3499 mL
    100 mM 0.0112 mL 0.0560 mL 0.1120 mL 0.2800 mL

    * Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.

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    Tariquidar methanesulfonate, hydrate Related Classifications

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    • 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:

    Tariquidar methanesulfonate,625375-83-9XR9576 methanesulfonate,P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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