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

Tariquidar (Synonyms: XR9576)

製品番号: HY-10550 純度: 97.55%
取扱説明書

Tariquidar is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1±0.9 nM).

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Tariquidar 構造式

Tariquidar 構造式

CAS 番号 : 206873-63-4

容量 価格(税別) 在庫状況 数量
10 mM * 1 mL in DMSO USD 71 在庫あり
Estimated Time of Arrival: December 31
5 mg USD 50 在庫あり
Estimated Time of Arrival: December 31
10 mg USD 90 在庫あり
Estimated Time of Arrival: December 31
50 mg USD 290 在庫あり
Estimated Time of Arrival: December 31
100 mg USD 490 在庫あり
Estimated Time of Arrival: December 31
200 mg   お問い合わせ  
500 mg   お問い合わせ  

* アイテムを追加する前、数量をご選択ください

カスタマーレビュー

Based on 21 publication(s) in Google Scholar

Other Forms of Tariquidar:

Top Publications Citing Use of Products

    Tariquidar purchased from MCE. Usage Cited in: Eur J Med Chem. 2017 Feb 15;127:586-598.

    Fluorescence ratio values in K562/DOX cells incubated with Rhd 123 in the absence (control) and in the presence of Verapamil (ver.) and Tariquidar (tar.) tested at 3.0 μM and 1.0 μM concentrations respectively.

    Tariquidar purchased from MCE. Usage Cited in: RSC Adv. 2016,6, 69083-69093.

    Western blot analysis on MCF-7/ADR cells after being treated by (A) control (without treatment), (B) free DOX, (C) CMC/CaCO3/DOX, (D) BCMC/CaCO3/DOX, (E) CMC/CaCO3/DOX/TQR, and (F) BCMC/CaCO3/DOX/TQR for 24 h.
    • 生物活性

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    • 参考文献

    • カスタマーレビュー

    製品説明

    Tariquidar is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1±0.9 nM).

    IC50 & Target

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

    体外実験

    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].

    体内実験

    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].

    臨床実験
    分子量

    646.73

    分子式

    C₃₈H₃₈N₄O₆

    CAS 番号

    206873-63-4

    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

    輸送条件

    Room temperature in continental US; may vary elsewhere.

    保管条件
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    溶剤 & 溶解度
    体外: 

    DMSO : ≥ 100 mg/mL (154.62 mM)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 1.5462 mL 7.7312 mL 15.4624 mL
    5 mM 0.3092 mL 1.5462 mL 3.0925 mL
    10 mM 0.1546 mL 0.7731 mL 1.5462 mL
    *Please refer to the solubility information to select the appropriate solvent.
    体内:
    • 1.

      Tariquidar (4 mg/mL) solution is prepared by adding it to a 5% DMSO-5% glucose solution[3].

    • 2.

      Tariquidar is freshly prepared on each experimental day in 2.5% aqueous dextrose solution[4].

    • 3.

      Tariquidar is dissolved in DMSO and adding heated 5% glucose solution (w/v) to a final DMSO concentration ≤ 2% (v/v)[5].

    参考文献
    細胞実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    動物実験
    [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 はこれらの方法の精度を確認していません。 こちらは参照専用です。

    参考文献
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    Keywords:

    TariquidarXR9576XR 9576XR-9576P-glycoproteinP-gpPgpMultidrug resistance protein 1MDR1ATP-binding cassette sub-family B member 1ABCB1Cluster of differentiation 243CD243Inhibitorinhibitorinhibit

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    製品名:
    Tariquidar
    製品番号:
    HY-10550
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