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產品描述： Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM) |
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靶點：
Kd: 5.1 nM (P-gp);P-gp |
體內研究：
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 |
參考文獻：
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 A 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. |
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溶解性：
DMSO : 25 mg/mL (38.66 mM; ultrasonic and adjust pH to 5 with HCl) DMSO : 16 mg/mL (24.74 mM; ultrasonic and warming and adjust pH to 3 with HCl and heat to 60°C) H2O : < 0.1 mg/mL (insoluble) |
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保存條件：
-20℃ |
配置溶液濃度參考：
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1mg |
5mg |
10mg |
| 1 mM |
1.546 ml |
7.731 ml |
15.462 ml |
| 5 mM |
0.309 ml |
1.546 ml |
3.092 ml |
| 10 mM |
0.155 ml |
0.773 ml |
1.546 ml |
| 50 mM |
0.031 ml |
0.155 ml |
0.309 ml |
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| 注意： |
部分產品我司僅能提供部分信息，我司不保證所提供信息的權威性，僅供客戶參考交流研究之用。 |
上海工商
北京