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Tariquidar 98%

Tariquidar

源葉(MedMol)
S80527
206873-63-4
C38H38N4O6
646.73
品牌 貨號(hào) 產(chǎn)品規(guī)格 價(jià)格(RMB) 庫(kù)存（上海） 北京 武漢 南京 購(gòu)買(mǎi)數(shù)量
源葉(MedMol) S80527-5mg 98% ￥320.00元 9 - - -
源葉(MedMol) S80527-10mg 98% ￥560.00元 6 - - -
源葉(MedMol) S80527-50mg 98% ￥1760.00元 4 - - -
源葉(MedMol) S80527-100mg 98% ￥3200.00元 1 - - -
產(chǎn)品介紹 參考文獻(xiàn)(2篇) 質(zhì)檢證書(shū)(COA) 摩爾濃度計(jì)算器 相關(guān)產(chǎn)品

產(chǎn)品介紹

Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM)
產(chǎn)品描述： Tariquidar (XR9576) is a potent and specific inhibitor of P-glycoprotein (P-gp) with the high affinity (Kd=5.1 nM)
靶點(diǎn)： Kd: 5.1 nM (P-gp);P-gp
體內(nèi)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(xiàn)：
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.
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)
保存條件： -20℃
配置溶液濃度參考：
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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摩爾濃度計(jì)算器

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